邻位取代苯的饱和生物等排体。
Saturated Bioisosteres of ortho-Substituted Benzenes.
机构信息
Enamine Ltd, Chervonotkatska 78, 02094, Kyiv, Ukraine.
"Institute for Single Crystals", National Academy of Science of Ukraine, Lenina Ave. 60, 61001, Kharkiv, Ukraine.
出版信息
Angew Chem Int Ed Engl. 2020 Nov 9;59(46):20515-20521. doi: 10.1002/anie.202004183. Epub 2020 Aug 18.
PMID:32662201
Abstract
Saturated bioisosteres of ortho-disubstituted benzenes (bicyclo[2.1.1]hexanes) were synthesized, characterized and validated. These cores were incorporated into the bioactive compounds Valsartan, Boskalid and Fluxapyroxad instead of the benzene ring. The saturated analogues showed a similar level of antifungal activity compared to that of Boskalid and Fluxapyroxad.
摘要
合成、表征并验证了邻位取代苯（双环[2.1.1]己烷）的饱和生物等排体。将这些核心结构引入到缬沙坦、波生坦和氟环唑等具有生物活性的化合物中，取代苯环。与波生坦和氟环唑相比，饱和类似物表现出相似水平的抗真菌活性。
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