Saturated Bioisosteres of <i>ortho</i>‐Substituted Benzenes
Aleksandr Denisenko, Pavel Garbuz, Svitlana V. Shishkina, Nataliya M. Voloshchuk, Pavel K. Mykhailiuk
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.
Topics & Concepts
BenzeneAntifungalChemistryRing (chemistry)Medicinal chemistryOrganic chemistryBiologyMicrobiologyOxidative Organic Chemistry ReactionsAsymmetric Synthesis and CatalysisOrganic Chemistry Cycloaddition Reactions