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Saturated Bioisosteres of ortho ‐Substituted Benzenes
Author(s) -
Denisenko Aleksandr,
Garbuz Pavel,
Shishkina Svetlana V.,
Voloshchuk Nataliya M.,
Mykhailiuk Pavel K.
Publication year - 2020
Publication title -
angewandte chemie
Language(s) - English
Resource type - Journals
eISSN - 1521-3757
pISSN - 0044-8249
DOI - 10.1002/ange.202004183
Subject(s) - benzene , chemistry , antifungal , ring (chemistry) , bicyclic molecule , benzene derivatives , medicinal chemistry , organic chemistry , chemical synthesis , medicine , biochemistry , dermatology , in vitro
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 .
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