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官能团反转作为农用化学品领域中一种有用的骨架跃迁工具。

Reversal of Functional Groups as a Useful Scaffold Hopping Tool in Agrochemistry.

机构信息

Chemical Research, Syngenta Crop Protection AG, Schaffhauserstrasse 101, CH-4332 Stein, Switzerland.

出版信息

J Agric Food Chem. 2022 Sep 14;70(36):11005-11010. doi: 10.1021/acs.jafc.1c08009. Epub 2022 Apr 5.

Abstract

Reverting the orientation of a functional group by exchanging molecular parts of it is an important scaffold hopping manipulation, as biologically active compounds and their analogs, which underwent such a transformation, are often similar in shape and physicochemical properties and therefore likely in their potency as well. This review will demonstrate, how the inversion of carboxamides, sulfonamides, carbamates, oximes, hydrazones, O,S-acetals, and ethers led to the discovery of highly active agrochemicals.

摘要

通过交换其分子部分来反转官能团的方向是一种重要的骨架跳跃操作,因为经历这种转化的生物活性化合物及其类似物在形状和物理化学性质上往往相似,因此它们的效力也可能相似。本综述将展示如何通过反转酰胺、磺酰胺、氨基甲酸酯、肟、腙、O,S-缩醛和醚的方向,发现高活性的农用化学品。

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