title: [Design, synthesis and evaluation of N-acyl-4-phenylthiazole-2-amines as acetylcholinesterase inhibitors].
abstract: N-Acyl-4-phenylthiazole-2-amines were designed and synthesized, moreover their effects on acetylcholinesterase activities were tested. N-Acyl-4-phenylthiazole-2-amines were prepared from substituted 2-bromo-1-acetophenones by three steps reaction, and their AChE inhibitory activities were measured by Ellman method in vitro. The results showed that the target compounds had a certain inhibitory activity on AChE in vitro. Among them, 8c was the best, and IC50 of 8c was 0.51 micromol x L(-1), better than that of rivastigmine and Huperzine-A. The inhibitory activities of N-acyl-4-phenylthiazole-2-amines on acetylcholinesterase are worth while to be further studied.
authors.forename: Zheng-Yue
authors.initials: ZY
authors.lastname: Ma
authors.forename: Qi
authors.initials: Q
authors.lastname: Yang
authors.forename: Yuan-Gong
authors.initials: YG
authors.lastname: Zhang
authors.forename: Jun-Jie
authors.initials: JJ
authors.lastname: Li
authors.forename: Geng-Liang
authors.initials: GL
authors.lastname: Yang
mesh_terms: D000110:Acetylcholinesterase / Q000378:metabolism; D000470:Alkaloids / Q000494:pharmacology; D000588:Amines / Q000138:chemical synthesis / Q000494:pharmacology*; D002800:Cholinesterase Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology*; D015195:Drug Design; D000068836:Rivastigmine / Q000494:pharmacology; D012717:Sesquiterpenes / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000494:pharmacology*
chemical_list: D000470:Alkaloids; D000588:Amines; D002800:Cholinesterase Inhibitors; D012717:Sesquiterpenes; D013844:Thiazoles; C050426:huperzine A; D000110:Acetylcholinesterase; D000068836:Rivastigmine