Design, synthesis and evaluation of N-acyl-4-phenylthiazole-2-amines as acetylcholinesterase inhibitors

N-Acyl-4-phenylthiazole-2-amines were designed and synthesized, moreover their effects onacetylcholinesterase 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 μmol·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.