Synthesis and antimicrobial evaluation of oxazole-1,4-naphthquinones

Abstract

Several routes for preparing oxazole nucleus fused to 1,4-naphthoquinone moiety were studied. Three new oxazole-1,4-naphthoquinone derivatives (4a-c) were prepared and evaluated against phatogenic bacteria. The use of ortho-ester methodology was found to be the best synthetic method for preparing these oxazoles, which showed very low antibacterial activity. The intermediate 2 showed a broad spectrum of activity comparable with oxacillin and vancomycin.