Design, synthesis and biological evaluation of organophosphorous-homodimers as dual binding site acetylcholinesterase inhibitors

R Xie, Q Zhao, T Zhang, J Fang, X Mei, J Ning…

Index: Xie, Ruliang; Zhao, Qianfei; Zhang, Tao; Fang, Jing; Mei, Xiangdong; Ning, Jun; Tang, Yun Bioorganic and Medicinal Chemistry, 2013 , vol. 21, # 1 p. 278 - 282

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Citation Number: 12

Abstract

The cluster effect is an effective strategy to explore new lead compounds, and has been successfully applied in rational drug design and screening. A series of novel organophosphorous-homodimers were designed and synthesized based on the dual-site structure characteristics of acetylcholinesterase (AChE). The compounds were evaluated in vitro for their inhibitory activity to AChE extracted from Drosophila melanogaster and ...