Chemical Research, Syngenta Crop Protection AG, Schaffhauserstrasse 101, CH-4332 Stein, Switzerland.
J Agric Food Chem. 2023 Nov 29;71(47):18123-18132. doi: 10.1021/acs.jafc.3c00997. Epub 2023 Apr 6.
Replacing one ring in a molecule by a different carba- or heterocycle is an important scaffold hopping manipulation, because biologically active compounds and their analogues, which underwent such a transformation, are often similar in size, shape, and physicochemical properties and, therefore, likely in their potency as well. This review will demonstrate, how isosteric ring exchange led to the discovery of highly active agrochemicals and which ring interchanges have proven to be most successful.
用不同的碳环或杂环取代分子中的一个环是一种重要的骨架跃迁操作,因为经历这种转化的生物活性化合物及其类似物在大小、形状和物理化学性质上往往相似,因此在效力上也可能相似。本综述将展示如何通过等排环交换发现高活性的农用化学品,以及哪些环交换已被证明是最成功的。