Saturated Bioisosteres of ortho-Substituted Benzenes

Angew. Chem. Int. Ed. 2020, 59 (46), 20515‑20521

DOI: 10.1002/anie.202004183

Denisenko A.; Garbuz P.; Shishkina S.; Voloshchuk N.; Mykhailiuk P.

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.