4.7 Article

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

Journal

BIOORGANIC & MEDICINAL CHEMISTRY
Volume 16, Issue 17, Pages 8294-8300

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2008.05.008

Keywords

ketoconazole; NO-donors; NONOates; diazeniumdiolates; nitric oxide; hybrids

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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. (C) 2008 Elsevier Ltd. All rights reserved.

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