title: Design, synthesis and evaluation of new thiazole-piperazines as acetylcholinesterase inhibitors.
abstract: In this study, some new 2-(4-substituted piperazine-1-yl)-N-[4-(2-methylthiazol-4-yl)phenyl]acetamide derivatives were synthesized. The synthesized compounds were screened for their anticholinesterase activity on acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes by in vitro Ellman's method. The structural elucidation of the compounds was performed by using IR, (1)H-NMR, (13)C-NMR and FAB(+)-MS spectral data and elemental analyses results. Biological assays revealed that at 0.1 µM concentration, the most active compounds against AChE were 5n, 5o and 5p that indicated 96.44, 99.83 and 89.70% inhibition rates, respectively. Besides, IC50 value of the compound 5o was determined as 0.011 µM, whereas IC50 value of standard drug donepezil was 0.054 µM. The synthesized compounds did not show any notable inhibitory activity against BChE.
authors.affiliation: Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Anadolu University , Eskişehir , Turkey.
authors.forename: Leyla
authors.initials: L
authors.lastname: Yurttaş
authors.forename: Zafer Asım
authors.initials: ZA
authors.lastname: Kaplancıklı
authors.forename: Yusuf
authors.initials: Y
authors.lastname: Özkay
mesh_terms: D000110:Acetylcholinesterase / Q000378:metabolism*; D002800:Cholinesterase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D015394:Molecular Structure; D010879:Piperazines / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D002800:Cholinesterase Inhibitors; D010879:Piperazines; D013844:Thiazoles; D000110:Acetylcholinesterase