Silicon-Containing Complex II Acaricides─Design, Synthesis, and Pharmacological Optimization,Journal of Agricultural and Food Chemistry

当前位置： X-MOL 学术 › J. Agric. Food Chem. › 论文详情

Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)

Silicon-Containing Complex II Acaricides─Design, Synthesis, and Pharmacological Optimization
Journal of Agricultural and Food Chemistry ( IF 5.7 ) Pub Date : 2022-05-16 , DOI: 10.1021/acs.jafc.2c00804
Cong Zhou ₁ , Xin Wang ₁ , Xiaocao Quan ₁ , Jiagao Cheng ₁ , Zhong Li ₁ , Peter Maienfisch _{1,

2}

Affiliation

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.

中文翻译：

含硅复合物 II 杀螨剂─设计、合成和药理学优化

生物等排体替代已被证明是生命科学研究中的一种强有力的策略。在这篇综述中，描述了碳-硅生物等排取代的一般方面及其在药物和作物保护研究中的应用。碳及其硅类似物具有相似的固有特性。在药物和杀虫剂中用硅代替碳已显示出对功效和选择性、物理化学性质和生物利用度产生积极影响，并且在许多情况下还可以消除或改善人类或环境安全性以及提供新颖性和新的知识产权。此外，还强调了碳-硅取代在寻找新的复杂 II 杀螨剂中的应用。这项研究导致了 sila-cyflumetofen 23a的发现以及其他与环氟美托芬的杀螨活性相匹配或超过的环氟美托芬含硅类似物。将讨论分子设计策略、合成方面、生物活性、计算建模工作和结构-活性关系。

更新日期：2022-05-16

点击分享查看原文

点击收藏

阅读更多本刊最新论文本刊介绍/投稿指南11