Design, one-pot synthesis, and evaluation of 7H-thiazolo3,2-b-1,2,4-triazin-7-one derivatives as dual binding site acetylcholinesterase inhibitors

摘要

In order to study the the structure-AChE inhibitory activity relationships of 7H-thiazolo[3,2-b]-1,2,4-triazin-7-one derivatives, the 7H-thiazolo[3,2-b][1,2,4]triazin-7-ones were designed by molecular docking, and readily prepared via a one-pot reaction in N-methyl pyrrolidone hydrosulfate ([Hnmp]HSO_4) lonic liquid. The study of AChE inhibitory activity was carried out using the Ellman colorimetric assay with huperzine-A as the positive control drug. Most of the target compounds exhibited more than 50% inhibition at 10μM.