Journal
CHEMISTRY-A EUROPEAN JOURNAL
Volume 14, Issue 8, Pages 2465-2481Publisher
WILEY-BLACKWELL
DOI: 10.1002/chem.200701237
Keywords
amphotericin B; antifungal agents; bioorganic chemistry; natural products; total synthesis
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Novel cationic amphotericin B derivatives as highly potent antifungal agents are reported. These semisynthetic derivatives of amphotericin B were elaborated through a series of modifications both on the nitrogen atom of the mycosamine and on the C-16 carboxylic acid moiety. The antifungal activity of the new conjugates was tested against Saccharomyces cerevisiae and also against nine different strains of Candida albicans and Candida glabrata, including an amphotericin resistant strain. High potency was observed in the case of polyamine derivatives bearing two 3-aminopropyl chains on the mycosamine. The evaluation of the biological properties also included the determination of the hemolytic activity of the compounds by measuring the EH(50) values.
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