Citrafungins A and B, two new fungal metabolite inhibitors of GGTase I with antifungal activity |
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| Authors: | Singh Sheo B Zink Deborah L Doss George A Polishook Jon D Ruby Carolyn Register Elizabeth Kelly Theresa M Bonfiglio Cynthia Williamson Joanne M Kelly Rosemarie |
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| Institution: | Merck Research Laboratories, P.O. Box 2000, Rahway, New Jersey 07065, USA. sheo_singh@merck.com |
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| Abstract: | structure: see text] Screening of natural products extracts led to the discovery of citrafungins A and B, two new fungal metabolites of the alkylcitrate family that are inhibitors of GGTase I of various pathogenic fungal species with IC(50) values of 2.5-15 microM. These compounds exhibited antifungal activities with MIC values of 0.40-55 microM. The isolation, structure elucidation, relative and absolute stereochemistry, and biological activities of citrafungins are described. |
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