Saturated Bioisosteres of ortho ‐Substituted Benzenes
2020; Wiley; Volume: 59; Issue: 46 Linguagem: Inglês
10.1002/anie.202004183
ISSN1521-3773
AutoresAleksandr Denisenko, Pavel Garbuz, Svitlana V. Shishkina, Nataliya M. Voloshchuk, Pavel K. Mykhailiuk,
Tópico(s)Organic Chemistry Cycloaddition Reactions
ResumoAbstract 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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