Synthesis and biological evaluation of nectriatide derivatives, potentiators of amphotericin B activity.

J Antibiot (Tokyo)

Microbial Chemistry and Medical Research Laboratories, Graduate School of Pharmaceutical Sciences, Kitasato University, 5-9-1 Shirokane, Minato-ku, Tokyo, 108-8641, Japan.

Published: April 2024

Nectriatide 1a, a naturally occurring cyclic tetrapeptide, has been reported to a potentiator of amphotericin B (AmB) activity. In order to elucidate its structure-activity relationships, we synthesized nectriatide derivatives with different amino acids in solution-phase synthesis and evaluated AmB-potentiating activity against Candida albicans. Among them, C-and N-terminal protected linear peptides were found to show the most potent AmB-potentiating activity.

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http://dx.doi.org/10.1038/s41429-023-00700-4DOI Listing

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