文献类型：期刊文献

英文题名：Silicon-Containing Complex II Acaricides-Design, Synthesis, and Pharmacological Optimization

作者：Zhou, Cong[1];Wang, Xin[1];Quan, Xiaocao[1];Cheng, Jiagao[1];Li, Zhong[1];Maienfisch, Peter[1,2]

机构：[1]East China Univ Sci & Technol, Sch Pharm, Shanghai Key Lab Chem Biol, Shanghai 200237, Peoples R China;[2]CreInSol MCB, CH-4118 Rodersdorf, Switzerland

年份：2022

卷号：70

期号：36

起止页码：11063

外文期刊名：JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY

收录：;EI(收录号：20222212184317);WOS:【SCI-EXPANDED(收录号:WOS:000821596300001)】；

语种：英文

外文关键词：carbon-silicon bioisosteric replacements; silicon-containing drugs and pesticides; complex II acaricides; cyflumetofen; structure-activity relationship; mode of action; computational modeling

摘要：Bioisosteric replacement has been proven to be a powerful strategy in life science research. In this review, general aspects of carbon-silicon bioisosteric substitution and its applications in pharmaceutical and crop protection research are described. Carbon and their silicon analogues possess similar intrinsic properties. Replacing carbon with silicon in pharmaceuticals and pesticides has shown to result in positive effects on efficacy and selectivity, physicochemical properties, and bioavailability and also to eliminate or improve human or environmental safety properties as well as to provide novelty and new intellectual property in many cases. Furthermore, the application of carbon-silicon substitution in the search for new complex II acaricides is highlighted. This research led to the discovery of sila-cyflumetofen 23a and other silicon-containing analogues of cyflumetofen that match or exceed the acaricidal activity of cyflumetofen. The molecular design strategy, synthetic aspects, biological activity, computational modeling work, and structure-activity relationships will be discussed.