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Tytuł pozycji:

Synthesis and biological evaluation of some thiazole derivatives as new cholinesterase inhibitors.

Tytuł:
Synthesis and biological evaluation of some thiazole derivatives as new cholinesterase inhibitors.
Autorzy:
Turan-Zitouni G; Department of Pharmaceutical Chemistry, Anadolu University, Faculty of Pharmacy, Eskişehir, Turkey.
Ozdemir A
Kaplancikli ZA
Altintop MD
Temel HE
Çiftçi GA
Źródło:
Journal of enzyme inhibition and medicinal chemistry [J Enzyme Inhib Med Chem] 2013 Jun; Vol. 28 (3), pp. 509-14. Date of Electronic Publication: 2012 Feb 03.
Typ publikacji:
Journal Article
Język:
English
Imprint Name(s):
Original Publication: Basingstoke, UK : Taylor & Francis, c2002-
MeSH Terms:
Cholinesterase Inhibitors/*chemical synthesis
Cholinesterase Inhibitors/*pharmacology
Thiazoles/*chemistry
Acetylcholinesterase/metabolism ; Animals ; Butyrylcholinesterase/metabolism ; Chemistry Techniques, Synthetic ; Cholinesterase Inhibitors/chemistry ; Dose-Response Relationship, Drug ; Drug Evaluation, Preclinical/methods ; Magnetic Resonance Spectroscopy ; Mice ; Molecular Structure ; NIH 3T3 Cells/drug effects ; Structure-Activity Relationship
Substance Nomenclature:
0 (Cholinesterase Inhibitors)
0 (Thiazoles)
EC 3.1.1.7 (Acetylcholinesterase)
EC 3.1.1.8 (Butyrylcholinesterase)
Entry Date(s):
Date Created: 20120204 Date Completed: 20130912 Latest Revision: 20171116
Update Code:
20240104
DOI:
10.3109/14756366.2011.653355
PMID:
22299580
Czasopismo naukowe
In the present study, some thiazole derivatives were synthesized via the ring closure reaction of 1-[2-(2-oxobenzo[d]thiazol-3(2H)-yl)acetyl]thiosemicarbazide with various phenacyl bromides. The chemical structures of the compounds were elucidated by (1)H NMR, (13)C NMR and mass spectral data and elemental analyses. Each derivative was evaluated for its ability to inhibit acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) using a modification of Ellman's spectrophotometric method. The compounds were also investigated for their cytotoxic properties using MTT assay. The most potent AChE inhibitor was found as compound 4e (IC(50) = 25.5 ± 2.12 µg/mL) followed by compounds 4i (IC(50) = 38.50 ± 2.12 µg/mL), 4c (IC(50) = 58.42 ± 3.14 µg/mL) and 4g (IC(50) = 68 ± 2.12 µg/mL) when compared with eserine (IC(50) = 0.025 ± 0.01 µg/mL). Effective compounds on AChE exhibited weak inhibition on BuChE (IC(50) > 80 µg/mL). MTT assay indicated that the cytotoxic dose (IC(50) = 71.67 ± 7.63 µg/mL) of compound 4e was higher than its effective dose.
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