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Wyszukujesz frazę ""Thiazoles"" wg kryterium: Temat


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Tytuł :
Design, synthesis and biological evaluation of novel thiazole-naphthalene derivatives as potential anticancer agents and tubulin polymerisation inhibitors.
Autorzy :
Wang G; State Key Laboratory of Functions and Applications of Medicinal Plants, Guizhou Provincial Key Laboratory of Pharmaceutics, Guizhou Medical University, Guiyang, China.
Liu W; State Key Laboratory of Functions and Applications of Medicinal Plants, Guizhou Provincial Key Laboratory of Pharmaceutics, Guizhou Medical University, Guiyang, China.; School of Pharmacy, Guizhou Medical University, Guiyang, China.
Fan M; State Key Laboratory of Functions and Applications of Medicinal Plants, Guizhou Provincial Key Laboratory of Pharmaceutics, Guizhou Medical University, Guiyang, China.; School of Pharmacy, Guizhou Medical University, Guiyang, China.
He M; State Key Laboratory of Functions and Applications of Medicinal Plants, Guizhou Provincial Key Laboratory of Pharmaceutics, Guizhou Medical University, Guiyang, China.; School of Pharmacy, Guizhou Medical University, Guiyang, China.
Li Y; Engineering Research Center for the Development and Application of Ethnic Medicine and TCM (Ministry of Education), Guizhou Medical University, Guiyang, China.
Peng Z; College of Food Science and Technology, Shanghai Ocean University, Shanghai, China.
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Źródło :
Journal of enzyme inhibition and medicinal chemistry [J Enzyme Inhib Med Chem] 2021 Dec; Vol. 36 (1), pp. 1694-1702.
Typ publikacji :
Journal Article
MeSH Terms :
Drug Design*
Antineoplastic Agents/*pharmacology
Naphthalenes/*pharmacology
Thiazoles/*pharmacology
Tubulin/*metabolism
Tubulin Modulators/*pharmacology
Antineoplastic Agents/chemical synthesis ; Antineoplastic Agents/chemistry ; Apoptosis/drug effects ; Cell Line, Tumor ; Cell Proliferation/drug effects ; Dose-Response Relationship, Drug ; Drug Screening Assays, Antitumor ; Humans ; Molecular Docking Simulation ; Molecular Structure ; Naphthalenes/chemical synthesis ; Naphthalenes/chemistry ; Polymerization/drug effects ; Structure-Activity Relationship ; Thiazoles/chemical synthesis ; Thiazoles/chemistry ; Tubulin Modulators/chemical synthesis ; Tubulin Modulators/chemistry
Czasopismo naukowe
Tytuł :
Discovery of first-in-class imidazothiazole-based potent and selective ErbB4 (HER4) kinase inhibitors.
Autorzy :
Zaraei SO; Center for Biomaterials, Korea Institute of Science and Technology, PO Box 131, Cheongryang, Seoul, 130-650, Republic of Korea; Department of Biomolecular Science, Korea University of Science and Technology, 113 Gwahangno, Yuseong-gu, Daejeon, 305-333, Republic of Korea.
Sbenati RM; Sharjah Institute for Medical Research, University of Sharjah, Sharjah, 27272, United Arab Emirates.
Alach NN; Sharjah Institute for Medical Research, University of Sharjah, Sharjah, 27272, United Arab Emirates.
Anbar HS; Department of Clinical Pharmacy and Pharmacotherapeutics, Dubai Pharmacy College for Girls, Dubai, 19099, United Arab Emirates. Electronic address: .
El-Gamal R; Department of Medical Biochemistry, Faculty of Medicine, University of Mansoura, Mansoura, 35516, Egypt.
Tarazi H; Sharjah Institute for Medical Research, University of Sharjah, Sharjah, 27272, United Arab Emirates; Department of Medicinal Chemistry, College of Pharmacy, University of Sharjah, Sharjah, 27272, United Arab Emirates.
Shehata MK; Sharjah Institute for Medical Research, University of Sharjah, Sharjah, 27272, United Arab Emirates.
Abdel-Maksoud MS; Medicinal & Pharmaceutical Chemistry Department, Pharmaceutical and Drug Industries Research Division, National Research Centre NRC (ID: 60014618)), Dokki, Giza, 12622, Egypt.
Oh CH; Center for Biomaterials, Korea Institute of Science and Technology, PO Box 131, Cheongryang, Seoul, 130-650, Republic of Korea; Department of Biomolecular Science, Korea University of Science and Technology, 113 Gwahangno, Yuseong-gu, Daejeon, 305-333, Republic of Korea.
El-Gamal MI; Sharjah Institute for Medical Research, University of Sharjah, Sharjah, 27272, United Arab Emirates; Department of Medicinal Chemistry, College of Pharmacy, University of Sharjah, Sharjah, 27272, United Arab Emirates; Department of Medicinal Chemistry, Faculty of Pharmacy, University of Mansoura, Mansoura, 35516, Egypt. Electronic address: .
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Źródło :
European journal of medicinal chemistry [Eur J Med Chem] 2021 Nov 15; Vol. 224, pp. 113674. Date of Electronic Publication: 2021 Jun 29.
Typ publikacji :
Journal Article
MeSH Terms :
Protein Kinase Inhibitors/*chemistry
Receptor, ErbB-4/*antagonists & inhibitors
Thiazoles/*chemistry
Binding Sites ; Catalytic Domain ; Cell Line, Tumor ; Cell Proliferation/drug effects ; Drug Design ; Drug Screening Assays, Antitumor ; Humans ; Imidazoles/chemistry ; Molecular Docking Simulation ; Protein Kinase Inhibitors/metabolism ; Protein Kinase Inhibitors/pharmacology ; Proto-Oncogene Proteins B-raf/antagonists & inhibitors ; Proto-Oncogene Proteins B-raf/metabolism ; Receptor, ErbB-4/metabolism ; Structure-Activity Relationship ; Thiazoles/metabolism ; Thiazoles/pharmacology
Czasopismo naukowe
Tytuł :
Monotherapy with mirabegron had a better tolerance than the anticholinergic agents on overactive bladder: A systematic review and meta-analysis.
Autorzy :
Yi W; Urological Department, The Affiliated Hospital of Chengdu University, Chengdu, Sichuan, China.
Yang Y
Yang J
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Źródło :
Medicine [Medicine (Baltimore)] 2021 Oct 15; Vol. 100 (41), pp. e27469.
Typ publikacji :
Journal Article; Meta-Analysis; Systematic Review
MeSH Terms :
Acetanilides/*therapeutic use
Adrenergic beta-3 Receptor Agonists/*therapeutic use
Cholinergic Antagonists/*therapeutic use
Thiazoles/*therapeutic use
Urinary Bladder, Overactive/*drug therapy
Acetanilides/administration & dosage ; Acetanilides/adverse effects ; Adrenergic beta-3 Receptor Agonists/administration & dosage ; Adrenergic beta-3 Receptor Agonists/adverse effects ; Adult ; Aged ; Aged, 80 and over ; Case-Control Studies ; Cholinergic Antagonists/adverse effects ; Constipation/chemically induced ; Constipation/epidemiology ; Female ; Humans ; Hypertension/chemically induced ; Hypertension/epidemiology ; Male ; Middle Aged ; Outcome Assessment, Health Care ; Randomized Controlled Trials as Topic ; Safety ; Tachycardia/chemically induced ; Tachycardia/epidemiology ; Thiazoles/administration & dosage ; Thiazoles/adverse effects ; Urinary Tract Infections/chemically induced ; Urinary Tract Infections/epidemiology ; Vision, Low/chemically induced ; Vision, Low/epidemiology ; Xerostomia/chemically induced ; Xerostomia/epidemiology
Czasopismo naukowe
Tytuł :
Comparative study of two isothiazolinone biocides, 1,2-benzisothiazolin-3-one (BIT) and 4,5-dichloro-2-n-octyl-isothiazolin-3-one (DCOIT), on barrier function and mitochondrial bioenergetics using murine brain endothelial cell line (bEND.3).
Autorzy :
Kim D; College of Pharmacy Institute of Pharmaceutical Science and Technology, Hanyang University, Ansan, Korea.
Kim EH; College of Pharmacy Institute of Pharmaceutical Science and Technology, Hanyang University, Ansan, Korea.
Bae ON; College of Pharmacy Institute of Pharmaceutical Science and Technology, Hanyang University, Ansan, Korea.
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Źródło :
Journal of toxicology and environmental health. Part A [J Toxicol Environ Health A] 2021 Nov 17; Vol. 84 (22), pp. 932-943. Date of Electronic Publication: 2021 Jul 27.
Typ publikacji :
Comparative Study; Journal Article; Research Support, Non-U.S. Gov't
MeSH Terms :
Blood-Brain Barrier/*drug effects
Disinfectants/*toxicity
Mitochondria/*drug effects
Thiazoles/*toxicity
Animals ; Blood-Brain Barrier/metabolism ; Cell Line ; Disinfectants/chemistry ; Endothelial Cells/drug effects ; Endothelial Cells/metabolism ; Energy Metabolism/drug effects ; Glutathione/metabolism ; Membrane Potential, Mitochondrial/drug effects ; Mice ; Mitochondria/metabolism ; Oxygen Consumption/drug effects ; Reactive Oxygen Species/metabolism ; Thiazoles/chemistry
Czasopismo naukowe
Tytuł :
Novel chalcone-conjugated, multi-flexible end-group coumarin thiazole hybrids as potential antibacterial repressors against methicillin-resistant Staphylococcus aureus.
Autorzy :
Hu Y; Sauvage Laboratory for Smart Materials, Harbin Institute of Technology (Shenzhen), Shenzhen, 518055, China; Shenzhen Key Laboratory of Flexible Printed Electronics Technology, School of Materials Science and Engineering, Harbin Institute of Technology, Shenzhen, 518055, China.
Hu C; Dongguan School Affiliated to South China Normal University, Dongguan, 523755, China.
Pan G; Sauvage Laboratory for Smart Materials, Harbin Institute of Technology (Shenzhen), Shenzhen, 518055, China; Shenzhen Key Laboratory of Flexible Printed Electronics Technology, School of Materials Science and Engineering, Harbin Institute of Technology, Shenzhen, 518055, China.
Yu C; Sauvage Laboratory for Smart Materials, Harbin Institute of Technology (Shenzhen), Shenzhen, 518055, China; Shenzhen Key Laboratory of Flexible Printed Electronics Technology, School of Materials Science and Engineering, Harbin Institute of Technology, Shenzhen, 518055, China.
Ansari MF; School of Chemistry and Chemical Engineering, Southwest University, Chongqing, 400715, China.
Yadav Bheemanaboina RR; Sokol Institute for Pharmaceutical Life Sciences, Department of Chemistry and Biochemistry, Montclair State University, New Jersey, 07043, USA.
Cheng Y; School of Chemistry and Chemical Engineering, Southeast University, Nanjing, 211189, China.
Zhou C; Dongguan School Affiliated to South China Normal University, Dongguan, 523755, China. Electronic address: .
Zhang J; Sauvage Laboratory for Smart Materials, Harbin Institute of Technology (Shenzhen), Shenzhen, 518055, China; Shenzhen Key Laboratory of Flexible Printed Electronics Technology, School of Materials Science and Engineering, Harbin Institute of Technology, Shenzhen, 518055, China. Electronic address: .
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Źródło :
European journal of medicinal chemistry [Eur J Med Chem] 2021 Oct 15; Vol. 222, pp. 113628. Date of Electronic Publication: 2021 Jun 09.
Typ publikacji :
Journal Article
MeSH Terms :
Anti-Bacterial Agents/*pharmacology
Chalcones/*pharmacology
Coumarins/*pharmacology
Methicillin-Resistant Staphylococcus aureus/*drug effects
Thiazoles/*pharmacology
Animals ; Anti-Bacterial Agents/chemical synthesis ; Anti-Bacterial Agents/chemistry ; Cell Line ; Chalcones/chemistry ; Coumarins/chemistry ; Dose-Response Relationship, Drug ; Humans ; Mice ; Microbial Sensitivity Tests ; Molecular Docking Simulation ; Molecular Structure ; Structure-Activity Relationship ; Thiazoles/chemistry
Czasopismo naukowe
Tytuł :
Acyclic nucleoside phosphonates with 2-aminothiazole base as inhibitors of bacterial and mammalian adenylate cyclases.
Autorzy :
Břehová P; Institute of Organic Chemistry and Biochemistry, The Czech Academy of Sciences, 16610, Prague 6, Czech Republic.
Chaloupecká E; Institute of Organic Chemistry and Biochemistry, The Czech Academy of Sciences, 16610, Prague 6, Czech Republic; Department of Organic Chemistry, Faculty of Science, Charles University, Hlavova 8, 128 43, Prague 2, Czech Republic.
Česnek M; Institute of Organic Chemistry and Biochemistry, The Czech Academy of Sciences, 16610, Prague 6, Czech Republic.
Skácel J; Institute of Organic Chemistry and Biochemistry, The Czech Academy of Sciences, 16610, Prague 6, Czech Republic.
Dračínský M; Institute of Organic Chemistry and Biochemistry, The Czech Academy of Sciences, 16610, Prague 6, Czech Republic.
Tloušťová E; Institute of Organic Chemistry and Biochemistry, The Czech Academy of Sciences, 16610, Prague 6, Czech Republic.
Mertlíková-Kaiserová H; Institute of Organic Chemistry and Biochemistry, The Czech Academy of Sciences, 16610, Prague 6, Czech Republic.
Soto-Velasquez MP; Department of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy, Purdue University, 575 Stadium Mall Drive, West Lafayette, IN, 47907, USA.
Watts VJ; Department of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy, Purdue University, 575 Stadium Mall Drive, West Lafayette, IN, 47907, USA. Electronic address: .
Janeba Z; Institute of Organic Chemistry and Biochemistry, The Czech Academy of Sciences, 16610, Prague 6, Czech Republic. Electronic address: .
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Źródło :
European journal of medicinal chemistry [Eur J Med Chem] 2021 Oct 15; Vol. 222, pp. 113581. Date of Electronic Publication: 2021 May 28.
Typ publikacji :
Journal Article
MeSH Terms :
Adenylate Cyclase Toxin/*antagonists & inhibitors
Adenylyl Cyclase Inhibitors/*pharmacology
Anti-Bacterial Agents/*pharmacology
Organophosphonates/*pharmacology
Thiazoles/*pharmacology
Adenylate Cyclase Toxin/metabolism ; Adenylyl Cyclase Inhibitors/chemical synthesis ; Adenylyl Cyclase Inhibitors/chemistry ; Animals ; Anti-Bacterial Agents/chemical synthesis ; Anti-Bacterial Agents/chemistry ; Bacillus anthracis/drug effects ; Bordetella pertussis/drug effects ; Bordetella pertussis/enzymology ; Cell Line ; Dose-Response Relationship, Drug ; Humans ; Mice ; Microbial Sensitivity Tests ; Molecular Structure ; Neuralgia/drug therapy ; Organophosphonates/chemistry ; Structure-Activity Relationship ; Thiazoles/chemistry
Czasopismo naukowe
Tytuł :
Alpelisib administration reduced lymphatic malformations in a mouse model and in patients.
Autorzy :
Delestre F; Université de Paris, Paris, 75006, France.; INSERM U1151, Institut Necker-Enfants Malades, Paris, 75015, France.
Venot Q; Université de Paris, Paris, 75006, France.; INSERM U1151, Institut Necker-Enfants Malades, Paris, 75015, France.
Bayard C; Université de Paris, Paris, 75006, France.; INSERM U1151, Institut Necker-Enfants Malades, Paris, 75015, France.
Fraissenon A; INSERM U1151, Institut Necker-Enfants Malades, Paris, 75015, France.; Service d'Imagerie Pédiatrique, Hôpital Femme-Mère-Enfant, HCL, Bron, 69500, France.; Service de Radiologie Mère-Enfant, Hôpital Nord, Saint Etienne, 42000, France.
Ladraa S; Université de Paris, Paris, 75006, France.; INSERM U1151, Institut Necker-Enfants Malades, Paris, 75015, France.
Hoguin C; Université de Paris, Paris, 75006, France.; INSERM U1151, Institut Necker-Enfants Malades, Paris, 75015, France.
Chapelle C; INSERM U1151, Institut Necker-Enfants Malades, Paris, 75015, France.; Unité d'hypercroissance dysharmonieuse et anomalies vasculaires, Hôpital Necker-Enfants Malades, AP-HP, Paris, 75015, France.
Yamaguchi J; Université de Paris, Paris, 75006, France.; INSERM U1151, Institut Necker-Enfants Malades, Paris, 75015, France.
Cassaca R; Université de Paris, Paris, 75006, France.; INSERM U1151, Institut Necker-Enfants Malades, Paris, 75015, France.
Zerbib L; Université de Paris, Paris, 75006, France.; INSERM U1151, Institut Necker-Enfants Malades, Paris, 75015, France.
Magassa S; Université de Paris, Paris, 75006, France.; INSERM U1151, Institut Necker-Enfants Malades, Paris, 75015, France.
Morin G; Université de Paris, Paris, 75006, France.; INSERM U1151, Institut Necker-Enfants Malades, Paris, 75015, France.
Asnafi V; Université de Paris, Paris, 75006, France.; Laboratoire d'Oncohématologie, Hôpital Necker-Enfants Malades, AP-HP, Paris, 75015, France.
Villarese P; Laboratoire d'Oncohématologie, Hôpital Necker-Enfants Malades, AP-HP, Paris, 75015, France.
Kaltenbach S; Université de Paris, Paris, 75006, France.; Laboratoire d'Oncohématologie, Hôpital Necker-Enfants Malades, AP-HP, Paris, 75015, France.
Fraitag S; Département d'Anatomopathologie, Hôpital Necker-Enfants Malades, AP-HP, Paris, 75015, France.
Duong JP; Université de Paris, Paris, 75006, France.; Département d'Anatomopathologie, Hôpital Necker-Enfants Malades, AP-HP, Paris, 75015, France.
Broissand C; Pharmacie, Hôpital Necker-Enfants Malades, AP-HP, Paris, 75015, France.
Boccara O; Service de Dermatologie, Hôpital Necker-Enfants Malades, AP-HP, Paris, 75015, France.
Soupre V; Service de Chirurgie Maxillo-faciale Pédiatrique, Hôpital Necker-Enfants Malades, AP-HP, 75015, Paris, France.
Bonnotte B; Service de Médecine Interne et Immunologie Clinique, CHU Dijon Bourgogne, Dijon, 21000, France.
Chopinet C; Service d'Exploration Fonctionnelle Cardiovasculaire, CHU Lille, Lille, 59000, France.
Mirault T; Service de Médecine Vasculaire, Hôpital Européen Georges Pompidou, AP-HP, Paris, 75015, France.
Legendre C; Université de Paris, Paris, 75006, France.; Service de Néphrologie et Transplantation Adultes, Hôpital Necker-Enfants Malades, AP-HP, Paris, 75015, France.
Guibaud L; Service d'Imagerie Pédiatrique, Hôpital Femme-Mère-Enfant, HCL, Bron, 69500, France.
Canaud G; Université de Paris, Paris, 75006, France.; INSERM U1151, Institut Necker-Enfants Malades, Paris, 75015, France.; Unité d'hypercroissance dysharmonieuse et anomalies vasculaires, Hôpital Necker-Enfants Malades, AP-HP, Paris, 75015, France.; Service de Néphrologie et Transplantation Adultes, Hôpital Necker-Enfants Malades, AP-HP, Paris, 75015, France.
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Źródło :
Science translational medicine [Sci Transl Med] 2021 Oct 06; Vol. 13 (614), pp. eabg0809. Date of Electronic Publication: 2021 Oct 06.
Typ publikacji :
Journal Article; Research Support, Non-U.S. Gov't
MeSH Terms :
Thiazoles*
Animals ; Humans ; Mice
Czasopismo naukowe
Tytuł :
Discovery of novel purinylthiazolylethanone derivatives as anti-Candida albicans agents through possible multifaceted mechanisms.
Autorzy :
Sui YF; Institute of Bioorganic & Medicinal Chemistry, Key Laboratory of Luminescence Analysis and Molecular Sensing, Ministry of Education, School of Chemistry and Chemical Engineering, Southwest University, Chongqing, 400715, China.
Ansari MF; Institute of Bioorganic & Medicinal Chemistry, Key Laboratory of Luminescence Analysis and Molecular Sensing, Ministry of Education, School of Chemistry and Chemical Engineering, Southwest University, Chongqing, 400715, China.
Fang B; College of Pharmacy, National & Local Joint Engineering Research Center of Targeted and Innovative Therapeutics, Chongqing Key Laboratory of Kinase Modulators As Innovative Medicine, Chongqing University of Arts and Sciences, Chongqing, 402160, China. Electronic address: .
Zhang SL; School of Pharmaceutical Sciences, Chongqing Key Laboratory of Natural Product Synthesis and Drug Research, Chongqing University, Chongqing, 401331, China. Electronic address: .
Zhou CH; Institute of Bioorganic & Medicinal Chemistry, Key Laboratory of Luminescence Analysis and Molecular Sensing, Ministry of Education, School of Chemistry and Chemical Engineering, Southwest University, Chongqing, 400715, China. Electronic address: .
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Źródło :
European journal of medicinal chemistry [Eur J Med Chem] 2021 Oct 05; Vol. 221, pp. 113557. Date of Electronic Publication: 2021 May 25.
Typ publikacji :
Journal Article
MeSH Terms :
Antifungal Agents/*pharmacology
Candida albicans/*drug effects
Ethane/*pharmacology
Fungicides, Industrial/*pharmacology
Purines/*pharmacology
Thiazoles/*pharmacology
Antifungal Agents/chemical synthesis ; Antifungal Agents/chemistry ; Biofilms/drug effects ; Dose-Response Relationship, Drug ; Drug Discovery ; Drug Resistance, Fungal/drug effects ; Ethane/analogs & derivatives ; Ethane/chemistry ; Fungicides, Industrial/chemical synthesis ; Fungicides, Industrial/chemistry ; Microbial Sensitivity Tests ; Molecular Structure ; Purines/chemistry ; Structure-Activity Relationship ; Thiazoles/chemistry
Czasopismo naukowe
Tytuł :
Quantification of 2-aminothiazoline-4-carboxylic acid as a reliable marker of cyanide exposure using chemical derivatization followed by liquid chromatography-tandem mass spectrometry.
Autorzy :
Nishio T; Department of Legal Medicine, Teikyo University School of Medicine, 2-11-1, Kaga, Itabashi-ku, Tokyo 173-8605, Japan. Electronic address: .
Toukairin Y; Department of Legal Medicine, Teikyo University School of Medicine, 2-11-1, Kaga, Itabashi-ku, Tokyo 173-8605, Japan.
Hoshi T; Department of Legal Medicine, Teikyo University School of Medicine, 2-11-1, Kaga, Itabashi-ku, Tokyo 173-8605, Japan.
Arai T; Department of Legal Medicine, Teikyo University School of Medicine, 2-11-1, Kaga, Itabashi-ku, Tokyo 173-8605, Japan.
Nogami M; Department of Legal Medicine, Teikyo University School of Medicine, 2-11-1, Kaga, Itabashi-ku, Tokyo 173-8605, Japan.
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Źródło :
Journal of pharmaceutical and biomedical analysis [J Pharm Biomed Anal] 2022 Jan 05; Vol. 207, pp. 114429. Date of Electronic Publication: 2021 Oct 16.
Typ publikacji :
Journal Article
MeSH Terms :
Tandem Mass Spectrometry*
Thiazoles*
Chromatography, Liquid ; Cyanides ; Humans ; Spectrometry, Mass, Electrospray Ionization
Czasopismo naukowe
Tytuł :
Higher oral efficacy of ravuconazole in self-nanoemulsifying systems in shorter treatment in experimental chagas disease.
Autorzy :
Spósito PÁ; Laboratory of Pharmaceutics and Nanotechnology (LDGNano), Pharmacy School, Federal University of Ouro Preto, Minas Gerais, 35400-000, Brazil.
Mazzeti AL; Laboratory of Pharmaceutics and Nanotechnology (LDGNano), Pharmacy School, Federal University of Ouro Preto, Minas Gerais, 35400-000, Brazil; Laboratory of Cellular Biology, Oswaldo Cruz Institute, Oswaldo Cruz Foundation (Fiocruz), Rio de Janeiro, Brazil.
de Castro KCMP; Laboratory of Pharmaceutics and Nanotechnology (LDGNano), Pharmacy School, Federal University of Ouro Preto, Minas Gerais, 35400-000, Brazil; Laboratory of Parasitic Diseases, School of Medicine, Federal University of Ouro Preto, Minas Gerais, Brazil.
Mendes PF; Laboratory of Pharmaceutics and Nanotechnology (LDGNano), Pharmacy School, Federal University of Ouro Preto, Minas Gerais, 35400-000, Brazil.
Urbina JA; Venezuelan Institute for Scientific Research, Caracas, 1020A, Venezuela.
Bahia MT; Laboratory of Parasitic Diseases, School of Medicine, Federal University of Ouro Preto, Minas Gerais, Brazil.
Mosqueira VCF; Laboratory of Pharmaceutics and Nanotechnology (LDGNano), Pharmacy School, Federal University of Ouro Preto, Minas Gerais, 35400-000, Brazil. Electronic address: .
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Źródło :
Experimental parasitology [Exp Parasitol] 2021 Sep; Vol. 228, pp. 108142. Date of Electronic Publication: 2021 Aug 08.
Typ publikacji :
Journal Article
MeSH Terms :
Chagas Disease/*drug therapy
Thiazoles/*administration & dosage
Triazoles/*administration & dosage
Trypanosoma cruzi/*drug effects
Animals ; Chagas Disease/parasitology ; Emulsions ; Female ; Hep G2 Cells ; Humans ; Inhibitory Concentration 50 ; Mice ; Myocytes, Cardiac ; Nanostructures ; Rats ; Thiazoles/pharmacology ; Thiazoles/therapeutic use ; Thiazoles/toxicity ; Triazoles/pharmacology ; Triazoles/therapeutic use ; Triazoles/toxicity
Czasopismo naukowe
Tytuł :
Masitinib is a broad coronavirus 3CL inhibitor that blocks replication of SARS-CoV-2.
Autorzy :
Drayman N; Pritzker School for Molecular Engineering, The University of Chicago, Chicago, IL, USA. .
DeMarco JK; Center for Predictive Medicine for Biodefense and Emerging Infectious Diseases, University of Louisville, Louisville, KY, USA.
Jones KA; Department of Microbiology, Ricketts Laboratory, University of Chicago, Chicago, IL, USA.; Department of Chemistry, The University of Chicago, Chicago, IL, USA.
Azizi SA; Department of Ophthalmology and Visual Sciences, Illinois Eye and Ear Infirmary, College of Medicine, University of Illinois at Chicago, Chicago, IL, USA.; Department of Chemistry, The University of Chicago, Chicago, IL, USA.
Froggatt HM; Institut Pasteur, Viral Populations and Pathogenesis Unit, Centre National de la Recherche Scientifique UMR 3569, Paris, France.; Department of Molecular Genetics and Microbiology, Duke University, Durham, NC, USA.
Tan K; Department of Medicine, Division of Immunobiology, Larner College of Medicine, University of Vermont, Burlington, VT, USA.; Department of Molecular Genetics and Microbiology, Duke University, Durham, NC, USA.; Center for Structural Genomics of Infectious Diseases, Consortium for Advanced Science and Engineering, University of Chicago, Chicago, IL, USA.; Structural Biology Center, X-ray Science Division, Argonne National Laboratory, Argonne, IL, USA.
Maltseva NI; Department of Microbiology, Ricketts Laboratory, University of Chicago, Chicago, IL, USA.; Department of Molecular Genetics and Microbiology, Duke University, Durham, NC, USA.; Center for Structural Genomics of Infectious Diseases, Consortium for Advanced Science and Engineering, University of Chicago, Chicago, IL, USA.; Structural Biology Center, X-ray Science Division, Argonne National Laboratory, Argonne, IL, USA.
Chen S; Department of Microbiology, Ricketts Laboratory, University of Chicago, Chicago, IL, USA.; Cellular Screening Center, The University of Chicago, Chicago, IL, USA.
Nicolaescu V; Department of Microbiology, Ricketts Laboratory, University of Chicago, Chicago, IL, USA.
Dvorkin S; Department of Microbiology, Ricketts Laboratory, University of Chicago, Chicago, IL, USA.; Department of Microbiology, Ricketts Laboratory, University of Chicago, Chicago, IL, USA.
Furlong K; Department of Microbiology, Ricketts Laboratory, University of Chicago, Chicago, IL, USA.
Kathayat RS; Department of Microbiology, Ricketts Laboratory, University of Chicago, Chicago, IL, USA.; Department of Chemistry, The University of Chicago, Chicago, IL, USA.
Firpo MR; Pritzker School for Molecular Engineering, The University of Chicago, Chicago, IL, USA.; Department of Microbiology and Immunology, Stritch School of Medicine, Loyola University Chicago, Maywood, IL, USA.
Mastrodomenico V; Department of Microbiology and Immunology, Stritch School of Medicine, Loyola University Chicago, Maywood, IL, USA.
Bruce EA; Cellular Screening Center, The University of Chicago, Chicago, IL, USA.; Department of Medicine, Division of Immunobiology, Larner College of Medicine, University of Vermont, Burlington, VT, USA.; Department of Microbiology and Molecular Genetics, Larner College of Medicine, University of Vermont, Burlington, VT, USA.
Schmidt MM; Department of Medicine, Division of Immunobiology, Larner College of Medicine, University of Vermont, Burlington, VT, USA.; Department of Microbiology and Molecular Genetics, Larner College of Medicine, University of Vermont, Burlington, VT, USA.
Jedrzejczak R; Department of Molecular Genetics and Microbiology, Duke University, Durham, NC, USA.; Center for Structural Genomics of Infectious Diseases, Consortium for Advanced Science and Engineering, University of Chicago, Chicago, IL, USA.; Structural Biology Center, X-ray Science Division, Argonne National Laboratory, Argonne, IL, USA.
Muñoz-Alía MÁ; Department of Molecular Medicine, Mayo Clinic, Rochester, MN, USA.; Department of Molecular Medicine, Mayo Clinic, Rochester, MN, USA.
Schuster B; Department of Microbiology, Ricketts Laboratory, University of Chicago, Chicago, IL, USA.; Pritzker School for Molecular Engineering, The University of Chicago, Chicago, IL, USA.
Nair V; Department of Microbiology, Ricketts Laboratory, University of Chicago, Chicago, IL, USA.; Pritzker School for Molecular Engineering, The University of Chicago, Chicago, IL, USA.
Han KY; Center for Predictive Medicine for Biodefense and Emerging Infectious Diseases, University of Louisville, Louisville, KY, USA.; Department of Ophthalmology and Visual Sciences, Illinois Eye and Ear Infirmary, College of Medicine, University of Illinois at Chicago, Chicago, IL, USA.
O'Brien A; Department of Pharmaceutical Sciences, College of Pharmacy, Biophysics Core at Research Resources Center, University of Illinois at Chicago, Chicago, IL, USA.; Department of Microbiology and Immunology, Stritch School of Medicine, Loyola University Chicago, Maywood, IL, USA.
Tomatsidou A; Department of Medicine, Division of Immunobiology, Larner College of Medicine, University of Vermont, Burlington, VT, USA.; Department of Microbiology, Ricketts Laboratory, University of Chicago, Chicago, IL, USA.
Meyer B; Institut Pasteur, Viral Populations and Pathogenesis Unit, Centre National de la Recherche Scientifique UMR 3569, Paris, France.
Vignuzzi M; Structural Biology Center, X-ray Science Division, Argonne National Laboratory, Argonne, IL, USA.; Institut Pasteur, Viral Populations and Pathogenesis Unit, Centre National de la Recherche Scientifique UMR 3569, Paris, France.
Missiakas D; Department of Microbiology, Ricketts Laboratory, University of Chicago, Chicago, IL, USA.; Department of Microbiology, Ricketts Laboratory, University of Chicago, Chicago, IL, USA.
Botten JW; Cellular Screening Center, The University of Chicago, Chicago, IL, USA.; Department of Medicine, Division of Immunobiology, Larner College of Medicine, University of Vermont, Burlington, VT, USA.; Department of Microbiology and Molecular Genetics, Larner College of Medicine, University of Vermont, Burlington, VT, USA.; Vaccine Testing Center, Larner College of Medicine, University of Vermont, Burlington, VT, USA.
Brooke CB; Department of Microbiology and Molecular Genetics, Larner College of Medicine, University of Vermont, Burlington, VT, USA.; Department of Microbiology, University of Illinois at Urbana-Champaign, Urbana, IL, USA.; Carl R. Woese Institute for Genomic Biology, University of Illinois at Urbana-Champaign, Urbana, IL, USA.
Lee H; Vaccine Testing Center, Larner College of Medicine, University of Vermont, Burlington, VT, USA.; Department of Pharmaceutical Sciences, College of Pharmacy, Biophysics Core at Research Resources Center, University of Illinois at Chicago, Chicago, IL, USA.
Baker SC; Institut Pasteur, Viral Populations and Pathogenesis Unit, Centre National de la Recherche Scientifique UMR 3569, Paris, France.; Pritzker School for Molecular Engineering, The University of Chicago, Chicago, IL, USA.; Department of Microbiology and Immunology, Stritch School of Medicine, Loyola University Chicago, Maywood, IL, USA.
Mounce BC; Institut Pasteur, Viral Populations and Pathogenesis Unit, Centre National de la Recherche Scientifique UMR 3569, Paris, France.; Department of Biochemistry and Molecular Biology, The University of Chicago, Chicago, IL, USA.; Department of Microbiology and Immunology, Stritch School of Medicine, Loyola University Chicago, Maywood, IL, USA.
Heaton NS; Institut Pasteur, Viral Populations and Pathogenesis Unit, Centre National de la Recherche Scientifique UMR 3569, Paris, France.; Department of Molecular Genetics and Microbiology, Duke University, Durham, NC, USA.
Severson WE; Department of Chemistry, The University of Chicago, Chicago, IL, USA.; Center for Predictive Medicine for Biodefense and Emerging Infectious Diseases, University of Louisville, Louisville, KY, USA.
Palmer KE; Department of Microbiology, University of Illinois at Urbana-Champaign, Urbana, IL, USA.; Center for Predictive Medicine for Biodefense and Emerging Infectious Diseases, University of Louisville, Louisville, KY, USA.
Dickinson BC; Department of Microbiology, Ricketts Laboratory, University of Chicago, Chicago, IL, USA.; Department of Chemistry, The University of Chicago, Chicago, IL, USA.
Joachimiak A; Department of Molecular Genetics and Microbiology, Duke University, Durham, NC, USA.; Carl R. Woese Institute for Genomic Biology, University of Illinois at Urbana-Champaign, Urbana, IL, USA.; Center for Structural Genomics of Infectious Diseases, Consortium for Advanced Science and Engineering, University of Chicago, Chicago, IL, USA.; Structural Biology Center, X-ray Science Division, Argonne National Laboratory, Argonne, IL, USA.; Department of Biochemistry and Molecular Biology, The University of Chicago, Chicago, IL, USA.
Randall G; Carl R. Woese Institute for Genomic Biology, University of Illinois at Urbana-Champaign, Urbana, IL, USA.; Department of Microbiology, Ricketts Laboratory, University of Chicago, Chicago, IL, USA.
Tay S; Department of Microbiology, Ricketts Laboratory, University of Chicago, Chicago, IL, USA. .; Pritzker School for Molecular Engineering, The University of Chicago, Chicago, IL, USA.
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Źródło :
Science (New York, N.Y.) [Science] 2021 Aug 20; Vol. 373 (6557), pp. 931-936. Date of Electronic Publication: 2021 Jul 20.
Typ publikacji :
Journal Article; Research Support, N.I.H., Extramural; Research Support, U.S. Gov't, Non-P.H.S.
MeSH Terms :
Antiviral Agents/*pharmacology
COVID-19/*drug therapy
Coronavirus 3C Proteases/*antagonists & inhibitors
Coronavirus OC43, Human/*drug effects
Cysteine Proteinase Inhibitors/*pharmacology
SARS-CoV-2/*drug effects
Thiazoles/*pharmacology
A549 Cells ; Animals ; Antiviral Agents/chemistry ; Antiviral Agents/metabolism ; Antiviral Agents/therapeutic use ; COVID-19/virology ; Catalytic Domain ; Coronavirus 3C Proteases/chemistry ; Coronavirus 3C Proteases/metabolism ; Coronavirus OC43, Human/physiology ; Cysteine Proteinase Inhibitors/chemistry ; Cysteine Proteinase Inhibitors/metabolism ; HEK293 Cells ; Humans ; Inhibitory Concentration 50 ; Mice ; Mice, Transgenic ; Microbial Sensitivity Tests ; SARS-CoV-2/enzymology ; SARS-CoV-2/physiology ; Thiazoles/chemistry ; Thiazoles/metabolism ; Thiazoles/therapeutic use ; Viral Load/drug effects ; Virus Replication/drug effects
SCR Protocol :
COVID-19 drug treatment
Czasopismo naukowe
Tytuł :
Novel Anti-Melanogenic Compounds, ( Z )-5-(Substituted Benzylidene)-4-thioxothiazolidin-2-one Derivatives: In Vitro and In Silico Insights.
Autorzy :
Choi H; Laboratory of Medicinal Chemistry, College of Pharmacy, Pusan National University, Busan 46241, Korea.
Ryu IY; Laboratory of Medicinal Chemistry, College of Pharmacy, Pusan National University, Busan 46241, Korea.
Choi I; Laboratory of Medicinal Chemistry, College of Pharmacy, Pusan National University, Busan 46241, Korea.
Ullah S; Department of Molecular Medicine, The Scripps Research Institute, Jupiter, FL 33458, USA.
Jung HJ; Laboratory of Medicinal Chemistry, College of Pharmacy, Pusan National University, Busan 46241, Korea.
Park Y; Laboratory of Medicinal Chemistry, College of Pharmacy, Pusan National University, Busan 46241, Korea.
Jeong Y; Laboratory of Medicinal Chemistry, College of Pharmacy, Pusan National University, Busan 46241, Korea.
Hwang Y; Laboratory of Medicinal Chemistry, College of Pharmacy, Pusan National University, Busan 46241, Korea.
Hong S; Laboratory of Medicinal Chemistry, College of Pharmacy, Pusan National University, Busan 46241, Korea.
Yoon IS; Laboratory of Medicinal Chemistry, College of Pharmacy, Pusan National University, Busan 46241, Korea.
Yun H; Laboratory of Medicinal Chemistry, College of Pharmacy, Pusan National University, Busan 46241, Korea.
Kim MS; Laboratory of Medicinal Chemistry, College of Pharmacy, Pusan National University, Busan 46241, Korea.
Yoo JW; Laboratory of Medicinal Chemistry, College of Pharmacy, Pusan National University, Busan 46241, Korea.
Jung Y; Laboratory of Medicinal Chemistry, College of Pharmacy, Pusan National University, Busan 46241, Korea.
Chun P; College of Pharmacy, Inje University, Gyeongnam, Gimhae 50834, Korea.; Inje Institute of Pharmaceutical Sciences and Research, Inje University, Gyeongnam, Gimhae 50834, Korea.
Moon HR; Laboratory of Medicinal Chemistry, College of Pharmacy, Pusan National University, Busan 46241, Korea.
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Źródło :
Molecules (Basel, Switzerland) [Molecules] 2021 Aug 17; Vol. 26 (16). Date of Electronic Publication: 2021 Aug 17.
Typ publikacji :
Journal Article
MeSH Terms :
Enzyme Inhibitors/*chemistry
Enzyme Inhibitors/*pharmacology
Melanins/*biosynthesis
Thiazoles/*chemistry
Thiazoles/*pharmacology
Cell Line, Tumor ; Computer Simulation ; Enzyme Inhibitors/metabolism ; Humans ; Kinetics ; Molecular Docking Simulation ; Monophenol Monooxygenase/antagonists & inhibitors ; Monophenol Monooxygenase/chemistry ; Monophenol Monooxygenase/metabolism ; Protein Conformation ; Structure-Activity Relationship ; Thiazoles/metabolism
Czasopismo naukowe
Tytuł :
Novel imidazo[2,1-b]thiazole-based anticancer agents as potential focal adhesion kinase inhibitors: Synthesis, in silico and in vitro evaluation.
Autorzy :
Başoğlu F; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Istanbul University, Istanbul, Turkey.; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, European University of Lefke, Northern Cyprus, Turkey.
Ulusoy-Güzeldemirci N; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Istanbul University, Istanbul, Turkey.
Akalın-Çiftçi G; Department of Biochemistry, Faculty of Pharmacy, Anadolu University, Eskisehir, Turkey.
Çetinkaya S; Department of Molecular Biology and Genetics, Science Faculty, Sivas Cumhuriyet University, Sivas, Turkey.
Ece A; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Biruni University, Istanbul, Turkey.
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Źródło :
Chemical biology & drug design [Chem Biol Drug Des] 2021 Aug; Vol. 98 (2), pp. 270-282. Date of Electronic Publication: 2021 Jun 12.
Typ publikacji :
Journal Article; Research Support, Non-U.S. Gov't
MeSH Terms :
Antineoplastic Agents/*chemical synthesis
Focal Adhesion Protein-Tyrosine Kinases/*antagonists & inhibitors
Imidazoles/*chemistry
Protein Kinase Inhibitors/*chemistry
Thiazoles/*chemistry
Antineoplastic Agents/metabolism ; Antineoplastic Agents/pharmacology ; Apoptosis/drug effects ; Binding Sites ; Catalytic Domain ; Cell Line, Tumor ; Cell Survival/drug effects ; Focal Adhesion Protein-Tyrosine Kinases/metabolism ; Humans ; Imidazoles/metabolism ; Imidazoles/pharmacology ; Molecular Docking Simulation ; Protein Kinase Inhibitors/metabolism ; Protein Kinase Inhibitors/pharmacology ; Static Electricity ; Structure-Activity Relationship ; Thiazoles/metabolism ; Thiazoles/pharmacology
Czasopismo naukowe
Tytuł :
Phenylbenzothiazole derivatives: effects against a Trypanosoma cruzi infection and toxicological profiles.
Autorzy :
Martínez-Cerón S; Laboratory of Biochemistry Research, Escuela Superior de Medicina, Instituto Politécnico Nacional, Plan de San Luis y Díaz Mirón S/N, Casco de Santo Tomas, Miguel Hidalgo, 11340, Mexico City, Mexico.
Gutiérrez-Nágera NA; Instituto Nacional de Medicina Genómica - INMEGEN, Av. Periférico Sur No. 4809, Col. Arenal Tepepan, Tlalpan, 14610, Mexico City, Mexico.
Mirzaeicheshmeh E; Instituto Nacional de Medicina Genómica - INMEGEN, Av. Periférico Sur No. 4809, Col. Arenal Tepepan, Tlalpan, 14610, Mexico City, Mexico.
Cuevas-Hernández RI; Laboratory of Biochemistry Research, Escuela Superior de Medicina, Instituto Politécnico Nacional, Plan de San Luis y Díaz Mirón S/N, Casco de Santo Tomas, Miguel Hidalgo, 11340, Mexico City, Mexico. .
Trujillo-Ferrara JG; Laboratory of Biochemistry Research, Escuela Superior de Medicina, Instituto Politécnico Nacional, Plan de San Luis y Díaz Mirón S/N, Casco de Santo Tomas, Miguel Hidalgo, 11340, Mexico City, Mexico. .
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Źródło :
Parasitology research [Parasitol Res] 2021 Aug; Vol. 120 (8), pp. 2905-2918. Date of Electronic Publication: 2021 Jul 01.
Typ publikacji :
Journal Article
MeSH Terms :
Chagas Disease*/drug therapy
Nitroimidazoles*/therapeutic use
Nitroimidazoles*/toxicity
Thiazoles*/therapeutic use
Thiazoles*/toxicity
Trypanocidal Agents*/therapeutic use
Trypanocidal Agents*/toxicity
Trypanosoma cruzi*/drug effects
Animals ; Mice ; Toxicity Tests
Czasopismo naukowe
Tytuł :
Identification of Thiazoyl Guanidine Derivatives as Novel Antifungal Agents Inhibiting Ergosterol Biosynthesis for Treatment of Invasive Fungal Infections.
Autorzy :
Kato I; Shionogi Pharmaceutical Research Center, 1-1 Futaba-cho 3-chome, Toyonaka, Osaka 561-0825, Japan.
Ukai Y; Shionogi Pharmaceutical Research Center, 1-1 Futaba-cho 3-chome, Toyonaka, Osaka 561-0825, Japan.
Kondo N; Shionogi Pharmaceutical Research Center, 1-1 Futaba-cho 3-chome, Toyonaka, Osaka 561-0825, Japan.
Nozu K; Shionogi Pharmaceutical Research Center, 1-1 Futaba-cho 3-chome, Toyonaka, Osaka 561-0825, Japan.
Kimura C; Shionogi Pharmaceutical Research Center, 1-1 Futaba-cho 3-chome, Toyonaka, Osaka 561-0825, Japan.
Hashimoto K; Shionogi Pharmaceutical Research Center, 1-1 Futaba-cho 3-chome, Toyonaka, Osaka 561-0825, Japan.
Mizusawa E; Shionogi Pharmaceutical Research Center, 1-1 Futaba-cho 3-chome, Toyonaka, Osaka 561-0825, Japan.
Maki H; Shionogi Pharmaceutical Research Center, 1-1 Futaba-cho 3-chome, Toyonaka, Osaka 561-0825, Japan.
Naito A; Shionogi Pharmaceutical Research Center, 1-1 Futaba-cho 3-chome, Toyonaka, Osaka 561-0825, Japan.
Kawai M; Shionogi Pharmaceutical Research Center, 1-1 Futaba-cho 3-chome, Toyonaka, Osaka 561-0825, Japan.
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Źródło :
Journal of medicinal chemistry [J Med Chem] 2021 Jul 22; Vol. 64 (14), pp. 10482-10496. Date of Electronic Publication: 2021 Jun 30.
Typ publikacji :
Journal Article
MeSH Terms :
Antifungal Agents/*pharmacology
Ergosterol/*antagonists & inhibitors
Guanidine/*pharmacology
Invasive Fungal Infections/*drug therapy
Thiazoles/*pharmacology
Antifungal Agents/chemical synthesis ; Antifungal Agents/chemistry ; Aspergillus fumigatus/drug effects ; Dose-Response Relationship, Drug ; Ergosterol/biosynthesis ; Guanidine/analogs & derivatives ; Guanidine/chemistry ; Humans ; Invasive Fungal Infections/metabolism ; Microbial Sensitivity Tests ; Molecular Structure ; Structure-Activity Relationship ; Thiazoles/chemical synthesis ; Thiazoles/chemistry
Czasopismo naukowe
Tytuł :
Microwave-Assisted One Pot Three-Component Synthesis of Novel Bioactive Thiazolyl-Pyridazinediones as Potential Antimicrobial Agents against Antibiotic-Resistant Bacteria.
Autorzy :
Abu-Melha S; Department of Chemistry, Faculty of Science, King Khalid University, Abha 61413, Saudi Arabia.
Gomha SM; Chemistry Department, Faculty of Science, Cairo University, Giza 12613, Egypt.; Chemistry Department, Faculty of Science, Islamic University in Almadinah Almonawara, Almadinah Almonawara 42351, Saudi Arabia.
Abouzied AS; Pharmaceutical Chemistry Department, College of Pharmacy, University of Hail, Hail 81442, Saudi Arabia.; Pharmaceutical Chemistry Department, National Organization for Drug Control and Research (NODCAR), Giza 12311, Egypt.
Edrees MM; Department of Chemistry, Faculty of Science, King Khalid University, Abha 61413, Saudi Arabia.; Pharmaceutical Chemistry Department, National Organization for Drug Control and Research (NODCAR), Giza 12311, Egypt.
Abo Dena AS; Pharmaceutical Chemistry Department, National Organization for Drug Control and Research (NODCAR), Giza 12311, Egypt.; Faculty of Oral and Dental Medicine, Future University in Egypt (FUE), New Cairo 11835, Egypt.
Muhammad ZA; Pharmaceutical Chemistry Department, National Organization for Drug Control and Research (NODCAR), Giza 12311, Egypt.
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Źródło :
Molecules (Basel, Switzerland) [Molecules] 2021 Jul 13; Vol. 26 (14). Date of Electronic Publication: 2021 Jul 13.
Typ publikacji :
Journal Article
MeSH Terms :
Anti-Bacterial Agents/*chemical synthesis
Antifungal Agents/*chemical synthesis
Pyridazines/*chemical synthesis
Thiazoles/*chemical synthesis
Anti-Bacterial Agents/chemistry ; Anti-Bacterial Agents/pharmacology ; Antifungal Agents/chemistry ; Antifungal Agents/pharmacology ; Bacteria/drug effects ; Bacterial Infections/drug therapy ; Combinatorial Chemistry Techniques ; Drug Resistance, Bacterial ; Fungi/drug effects ; Humans ; Microwaves ; Molecular Docking Simulation ; Mycoses/drug therapy ; Pyridazines/chemistry ; Pyridazines/pharmacology ; Thiazoles/chemistry ; Thiazoles/pharmacology
Czasopismo naukowe
Tytuł :
Discovery of a Novel Triazolopyridine Derivative as a Tankyrase Inhibitor.
Autorzy :
Ryu H; Division of Radiation Biomedical Research, Korea Institute of Radiological & Medical Sciences, Seoul 01812, Korea.
Nam KY; Department of Research Center, Pharos I&BT Co., Ltd., Anyang 14059, Korea.
Kim HJ; Division of Radiation Biomedical Research, Korea Institute of Radiological & Medical Sciences, Seoul 01812, Korea.
Song JY; Division of Radiation Biomedical Research, Korea Institute of Radiological & Medical Sciences, Seoul 01812, Korea.
Hwang SG; Division of Radiation Biomedical Research, Korea Institute of Radiological & Medical Sciences, Seoul 01812, Korea.
Kim JS; Division of Radiation Biomedical Research, Korea Institute of Radiological & Medical Sciences, Seoul 01812, Korea.
Kim J; Laboratory of Biochemistry, Division of Life Sciences, Korea University, Seoul 02841, Korea.
Ahn J; Division of Radiation Biomedical Research, Korea Institute of Radiological & Medical Sciences, Seoul 01812, Korea.
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Źródło :
International journal of molecular sciences [Int J Mol Sci] 2021 Jul 08; Vol. 22 (14). Date of Electronic Publication: 2021 Jul 08.
Typ publikacji :
Journal Article
MeSH Terms :
Antineoplastic Agents*/chemistry
Antineoplastic Agents*/pharmacology
Colorectal Neoplasms*/drug therapy
Colorectal Neoplasms*/enzymology
Drug Discovery*
Enzyme Inhibitors*/chemistry
Enzyme Inhibitors*/pharmacology
Pyridines*/chemistry
Pyridines*/pharmacology
Thiazoles*/chemistry
Thiazoles*/pharmacology
Neoplasm Proteins/*antagonists & inhibitors
Tankyrases/*antagonists & inhibitors
Cell Line, Tumor ; Humans ; Neoplasm Proteins/metabolism ; Tankyrases/metabolism
Czasopismo naukowe
Tytuł :
Systemic efficacy on Cryptosporidium parvum infection of aminoxanide (RM-5061), a new amino-acid ester thiazolide prodrug of tizoxanide.
Autorzy :
Diawara EH; Laboratoire de Parasitologie-Mycologie, Rouen University Hospital and EA7510, University of Rouen, Rouen, France.
François A; Laboratoire d'Anatomo-Pathologie, Rouen University Hospital, Rouen, France.
Stachulski AV; Robert Robinson Laboratories, Department of Chemistry, University of Liverpool, LiverpoolL69 7ZD, UK.
Razakandrainibe R; Laboratoire de Parasitologie-Mycologie, Rouen University Hospital and EA7510, University of Rouen, Rouen, France.
Costa D; Laboratoire de Parasitologie-Mycologie, Rouen University Hospital and EA7510, University of Rouen, Rouen, France.
Favennec L; Laboratoire de Parasitologie-Mycologie, Rouen University Hospital and EA7510, University of Rouen, Rouen, France.
Rossignol JF; Romark Laboratories, L.C., Tampa, FL33609, USA.
Gargala G; Laboratoire de Parasitologie-Mycologie, Rouen University Hospital and EA7510, University of Rouen, Rouen, France.
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Źródło :
Parasitology [Parasitology] 2021 Jul; Vol. 148 (8), pp. 975-984. Date of Electronic Publication: 2021 Mar 29.
Typ publikacji :
Journal Article; Research Support, Non-U.S. Gov't
MeSH Terms :
Cryptosporidiosis/*drug therapy
Cryptosporidium parvum/*drug effects
Prodrugs/*therapeutic use
Thiazoles/*therapeutic use
Animals ; Cattle ; Cell Line/drug effects ; Cell Survival/drug effects ; Dose-Response Relationship, Drug ; Esters ; Feces/parasitology ; Female ; Gerbillinae ; Ileum/parasitology ; Ileum/pathology ; Inhibitory Concentration 50 ; Male ; Molecular Structure ; Prodrugs/chemistry ; Prodrugs/pharmacology ; Thiazoles/chemistry ; Thiazoles/pharmacology
Czasopismo naukowe
Tytuł :
Synthesis and BK channel-opening activity of 2-amino-1,3-thiazole derivatives.
Autorzy :
Qi XL; Department of Chemistry, Innovative Drug Research Center, College of Sciences, Shanghai University, Shanghai 200444, China.
Jo H; School of Life Sciences and National Leading Research Laboratory, Gwangju Institute of Science and Technology (GIST), Gwangju 61005, Republic of Korea.
Wang XY; Department of Chemistry, Innovative Drug Research Center, College of Sciences, Shanghai University, Shanghai 200444, China.
Ji TT; Department of Chemistry, Innovative Drug Research Center, College of Sciences, Shanghai University, Shanghai 200444, China.
Lin HX; Department of Chemistry, Innovative Drug Research Center, College of Sciences, Shanghai University, Shanghai 200444, China.
Park CS; School of Life Sciences and National Leading Research Laboratory, Gwangju Institute of Science and Technology (GIST), Gwangju 61005, Republic of Korea. Electronic address: .
Cui YM; Department of Chemistry, Innovative Drug Research Center, College of Sciences, Shanghai University, Shanghai 200444, China. Electronic address: .
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Źródło :
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2021 Jul 01; Vol. 43, pp. 128083. Date of Electronic Publication: 2021 May 06.
Typ publikacji :
Journal Article; Research Support, Non-U.S. Gov't
MeSH Terms :
Large-Conductance Calcium-Activated Potassium Channels/*metabolism
Thiazoles/*pharmacology
Dose-Response Relationship, Drug ; Humans ; Molecular Structure ; Structure-Activity Relationship ; Thiazoles/chemical synthesis ; Thiazoles/chemistry
Czasopismo naukowe

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