Saturated Bioisosteres of ortho-Substituted Benzenes.
Aleksandr DenisenkoPavel GarbuzSvetlana V ShishkinaNataliya M VoloshchukPavel K MykhailiukPublished in: Angewandte Chemie (International ed. in English) (2020)
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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