NO-donors. Part 171: Synthesis and antimicrobial activity of novel ketoconazole–NO-donor hybrid compounds

Novel hybrid compounds combining the antifungal drug ketoconazole with a diazen-1-ium-1,2-diolate or an organic nitrate moiety and the corresponding NO-donors without ketoconazole were synthesized and their activities against a broad variety of fungal strains were tested. Hybridization modifies the spectrum of antimicrobial activities and generally, the ketoconazole–NO-donor hybrids are more potent than ketoconazole. The NO-donors alone show insufficient effectiveness.

Antimicrobial activities of ketoconazole–NO-donor hybrids (MIC-values) against eight different fungal strains range from 0.6 to 1000 μM.Figure optionsDownload as PowerPoint slide