|
|||||
|
|
Saturated Bioisosteres of ortho-Substituted Benzenes |
|
| Authors: | Aleksandr Denisenko Pavel Garbuz Dr. Svetlana V. Shishkina Dr. Nataliya M. Voloshchuk Dr. Pavel K. Mykhailiuk |
| Affiliation: | 1. Enamine Ltd, Chervonotkatska 78, 02094 Kyiv, Ukraine;2. “Institute for Single Crystals”, National Academy of Science of Ukraine, Lenina Ave. 60, 61001 Kharkiv, Ukraine;3. National University of Life and Environmental Science of Ukraine, Heroiv Oborony 15, 03041 Kyiv, Ukraine |
| 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. |
| Keywords: | benzene bioisosteres bicyclo[1.1.1]pentanes bioisosterism conformational restriction ortho-substituted benzenes |