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Synthesis and In Vitro Biological Properties of Novel Cationic Derivatives of Amphotericin B
Author(s) -
Paquet Valérie,
Volmer Astrid A.,
Carreira Erick M.
Publication year - 2008
Publication title -
chemistry – a european journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.687
H-Index - 242
eISSN - 1521-3765
pISSN - 0947-6539
DOI - 10.1002/chem.200701237
Subject(s) - amphotericin b , moiety , chemistry , candida albicans , candida glabrata , in vitro , stereochemistry , cationic polymerization , antifungal , biological activity , microbiology and biotechnology , biochemistry , organic chemistry , biology
Novel cationic amphotericin B derivatives as highly potent antifungal agents are reported. These semi‐synthetic 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.