Synthesis, computational investigation and biological evaluation of α,α-difluoromethyl ketones embodying pyrazole and isoxazole nuclei as COX inhibitors

Abstract

Chemoselective, synthesis of pyrazole and isoxazole α,α-difluoromethyl ketones via nucleophilic transfer of −CHF2 moiety to Weinreb amides is reported. In silico docking on COX-1 or COX-2 and in vitro biological assays open new application for α,α-difluorinated ketones.