NO-donors. Part 17: 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.
Konter
Joerg
J
Institute of Pharmacy, Department of Pharmaceutical/Medicinal Chemistry, Friedrich-Schiller-University Jena, Philosophenweg 14, D-07743 Jena, Germany.
Möllmann
Ute
U
Lehmann
Jochen
J
D000935:Antifungal Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D001230:Aspergillus / Q000187:drug effects; D001487:Basidiomycota / Q000187:drug effects; D002175:Candida / Q000187:drug effects; D005658:Fungi / Q000187:drug effects*; D005670:Fusarium / Q000187:drug effects; D007654:Ketoconazole / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D009569:Nitric Oxide / Q000032:analysis; D020030:Nitric Oxide Donors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D010408:Penicillium chrysogenum / Q000187:drug effects; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
D000935:Antifungal Agents; D020030:Nitric Oxide Donors; D009569:Nitric Oxide; D007654:Ketoconazole