Saturated Bioisosteres of ortho‐Substituted Benzenes

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...

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Bibliographic Details
Published in:Angewandte Chemie International Edition 2020-11, Vol.59 (46), p.20515-20521
Main Authors: Denisenko, Aleksandr, Garbuz, Pavel, Shishkina, Svetlana V., Voloshchuk, Nataliya M., Mykhailiuk, Pavel K.
Format: Article
Language:English
Subjects:
Antifungal activity
Benzene
benzene bioisosteres
bicyclo[1.1.1]pentanes
Bioactive compounds
bioisosterism
conformational restriction
Fungicides
Hexanes
ortho-substituted benzenes
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Summary: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. 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.
ISSN:1433-7851
1521-3773
DOI:10.1002/anie.202004183