Identification of Inhibitors of Drug-Resistant Candida albicans Strains from a Library of Bicyclic Peptidomimetic Compounds

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• 作者：Andrea Trabocchi ; Claudia Mannino ; Fabrizio Machetti ; Flavia De Bernardis ; Silvia Arancia ; Roberto Cauda ; Antonio Cassone ; Antonio Guarna
• 刊名：Journal of Medicinal Chemistry
• 出版年：2010
• 出版时间：March 25, 2010
• 年：2010
• 卷：53
• 期：6
• 页码：2502-2509
• 全文大小：877K
• 年卷期：v.53,no.6(March 25, 2010)
• ISSN：1520-4804

文摘

The screening of a library of small molecule peptidomimetics toward secreted aspartic proteinase-2 (SAP2) of Candida albicans allowed us to identify two compounds that showed in vitro inhibitory potency comparable to pepstatin A. In an experimental model of vaginal candidiasis, the two candidate compounds were as active as a therapeutic dose of fluconazole. Importantly, this activity was fully preserved when the challenger was a fluconazole-resistant strain of the fungus. Altogether, our data demonstrate SAP2 as a valid C. albicans target for the development of new drugs against this important human pathogen.