Bivalent Organophosphorus Compounds-Synthesis and Acetylcholinesterase Inhibitory Activity

文献类型： 外文期刊

第一作者： Zhao, Qianfei

作者： Zhao, Qianfei;Zhang, Tao;Mei, Xiangdong;Yuan, Huizhu;Ning, Jun;Zhang, Ting

作者机构：

关键词： Cluster effect;bivalent organophosphorus compound;acetylcholinesterase inhibitory activity;dual binding

期刊名称：PHOSPHORUS SULFUR AND SILICON AND THE RELATED ELEMENTS （ 影响因子：1.082； 五年影响因子：0.859 ）

ISSN： 1042-6507

年卷期： 2013 年 188 卷 8 期

页码：

收录情况： SCI

摘要： A series of novel symmetric S,S-2,2-(ethane-1,2-diylbis(azanediyl)) bis(2-oxoethane-2,1-diyl) O,O,O,O-tetraethyl diphosphorodithioate derivatives (12) was designed and synthesized based on the cluster effect and the multiple binding sites of acetylcholinesterase (AChE). The structures of all the newly synthesized title compounds were characterized by H-1 and C-13 NMR as well as elemental analyses. Their inhibitory activities against AChE were tested, and compound 12b exhibited the best activity (6.60-fold higher than ethion). The results suggested that the compound would bind to the catalytic center and the narrow gorge of the AChE simultaneously. Supplementary materials are available for this article. Go to the publisher's online edition of Phosphorus, Sulfer, and Silicon and the Related Elements for the following free supplemental files: Additional table.

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