1,2-Disubstituted bicyclo[2.1.1]hexanes as saturated bioisosteres of ortho-substituted benzene

Literature Information

Publication Date 2023-10-27
DOI 10.1039/D3SC05121H
Impact Factor 9.825
Authors

Aleksandr Denisenko, Pavel Garbuz, Yelyzaveta Makovetska, Dmytro Lesyk, Rodion Korzh, Iryna V. Sadkova, Pavel K. Mykhailiuk


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Abstract

Bicyclo[2.1.1]hexanes have been synthesized, characterized, and biologically validated as saturated bioisosteres of the ortho-substituted benzene ring. The incorporation of the 1,2-disubstituted bicyclo[2.1.1]hexane core into the structure of fungicides boscalid (BASF), bixafen (Bayer CS), and fluxapyroxad (BASF) gave saturated patent-free analogs with high antifungal activity.

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