4.8 Article

Saturated Bioisosteres ofortho-Substituted Benzenes

期刊

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
卷 59, 期 46, 页码 20515-20521

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WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.202004183

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benzene bioisosteres; bicyclo[1; 1; 1]pentanes; bioisosterism; conformational restriction; ortho-substituted benzenes

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Saturated bioisosteres ofortho-disubstituted benzenes (bicyclo[2.1.1]hexanes) were synthesized, characterized and validated. These cores were incorporated into the bioactive compoundsValsartan, BoskalidandFluxapyroxadinstead of the benzene ring. The saturated analogues showed a similar level of antifungal activity compared to that ofBoskalidandFluxapyroxad.

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