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Short Paper | Regular issue | Vol 87, No. 12, 2013, pp.2607-2614
Published online, 8th November, 2013
DOI: 10.3987/COM-13-12820
Design, Synthesis, and Biological Evaluation of 7H-Thiazolo[3,2-b]-1,2,4-triazin-7-one Derivatives as Dual Binding Site Acetylcholinesterase Inhibitors

Si-Jie Liu, Li-Bo Cui, Hiu-Lan Xu, Tie-Ying Wang, Chun Hu,* Shuo Li, Huang-Quan Lin, and David Chicheong Wan

*Department of Organic Chemistry, Shenyang Pharmaceutical University, No. 103, Wenhua Road, Shenhe District, Shenyang 110016, China

Abstract

A series of 7H-thiazolo[3,2-b]-1,2,4-triazin-7-one derivatives were designed, synthesized and evaluated as dual binding site acetylcholinesterase inhibitors. The target compounds exhibited promising inhibitory activity for AChE. The structure-activity relationships were discussed and their binding conformation and simultaneous interactions mode were further clarified by the molecular docking studies.