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Tytuł pozycji:

Easy-To-Access Quinolone Derivatives Exhibiting Antibacterial and Anti-Parasitic Activities.

Tytuł :
Easy-To-Access Quinolone Derivatives Exhibiting Antibacterial and Anti-Parasitic Activities.
Autorzy :
Beteck RM; Centre of Excellence for Pharmaceutical Sciences, North-West University, Potchefstroom 2520, South Africa.
Jordaan A; SAMRC/NHLS/UCT Molecular Mycobacteriology Research Unit, Department of Pathology, Faculty of Health Sciences, Institute of Infectious Disease and Molecular Medicine, University of Cape Town, Cape Town 7925, South Africa.
Seldon R; SAMRC Drug Discovery and Development Research Unit, University of Cape Town, Cape Town 7700, South Africa.
Laming D; Centre for Chemico- and Biomedicinal Research, Rhodes University, Makhanda 6140, South Africa.
Hoppe HC; Centre for Chemico- and Biomedicinal Research, Rhodes University, Makhanda 6140, South Africa.; Department of Biochemistry and Microbiology, Faculty of Science, Rhodes University, Makhanda 6140, South Africa.
Warner DF; SAMRC/NHLS/UCT Molecular Mycobacteriology Research Unit, Department of Pathology, Faculty of Health Sciences, Institute of Infectious Disease and Molecular Medicine, University of Cape Town, Cape Town 7925, South Africa.; Wellcome Centre for Infectious Diseases Research in Africa, University of Cape Town, Cape Town 7925, South Africa.
Khanye SD; Centre for Chemico- and Biomedicinal Research, Rhodes University, Makhanda 6140, South Africa.; Division of Pharmaceutical Chemistry, Faculty of Pharmacy, Rhodes University, Makhanda 6140, South Africa.
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Źródło :
Molecules (Basel, Switzerland) [Molecules] 2021 Feb 20; Vol. 26 (4). Date of Electronic Publication: 2021 Feb 20.
Typ publikacji :
Journal Article
Język :
English
Imprint Name(s) :
Original Publication: Basel, Switzerland : MDPI, c1995-
MeSH Terms :
Anti-Bacterial Agents/*pharmacology
Antiprotozoal Agents/*pharmacology
Quinolones/*pharmacology
Acinetobacter baumannii/drug effects ; Anti-Bacterial Agents/chemical synthesis ; Anti-Bacterial Agents/chemistry ; Antiprotozoal Agents/chemical synthesis ; Antiprotozoal Agents/chemistry ; Dose-Response Relationship, Drug ; Microbial Sensitivity Tests ; Molecular Structure ; Parasitic Sensitivity Tests ; Plasmodium falciparum/drug effects ; Quinolones/chemical synthesis ; Quinolones/chemistry ; Staphylococcus aureus/drug effects ; Trypanosoma brucei brucei/drug effects
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Grant Information :
United Kingdom WT_ Wellcome Trust
Contributed Indexing :
Keywords: ESKAPE pathogens; anti-Mtb; human African trypanosomiasis; malaria; quinolones
Substance Nomenclature :
0 (Anti-Bacterial Agents)
0 (Antiprotozoal Agents)
0 (Quinolones)
Entry Date(s) :
Date Created: 20210306 Date Completed: 20210407 Latest Revision: 20210407
Update Code :
20210408
PubMed Central ID :
PMC7931078
DOI :
10.3390/molecules26041141
PMID :
33672753
Czasopismo naukowe
The cell wall of Mycobacterium tuberculosis ( Mtb ) has a unique structural organisation, comprising a high lipid content mixed with polysaccharides. This makes cell wall a formidable barrier impermeable to hydrophilic agents. In addition, during host infection, Mtb resides in macrophages within avascular necrotic granulomas and cavities, which shield the bacterium from the action of most antibiotics. To overcome these protective barriers, a new class of anti-TB agents exhibiting lipophilic character have been recommended by various reports in literature. Herein, a series of lipophilic heterocyclic quinolone compounds was synthesised and evaluated in vitro against pMSp12::GFP strain of Mtb, two protozoan parasites ( Plasmodium falciparum and Trypanosoma brucei brucei ) and against ESKAPE pathogens. The resultant compounds exhibited varied anti- Mtb activity with MIC 90 values in the range of 0.24-31 µM. Cross-screening against P. falciparum and T.b. brucei , identified several compounds with antiprotozoal activities in the range of 0.4-20 µM. Compounds were generally inactive against ESKAPE pathogens, with only compounds 8c , 8g and 13 exhibiting moderate to poor activity against S. aureus and A. baumannii .
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