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

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...

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Bibliographic Details
Published in:Journal of antibiotics 2024-04, Vol.77 (4), p.214-220
Main Authors: Nagai, Kenichiro, Kobayashi, Keisuke, Miyake, Ryosuke, Sato, Yukino, Seki, Reiko, Fukuda, Takashi, Yagi, Akiho, Uchida, Ryuji, Ohshiro, Taichi, Tomoda, Hiroshi
Format: Article
Language:English
Subjects:
631/92/349
631/92/349/977
Amino acids
Amphotericin B
Amphotericin B - chemistry
Antibiotics
Antifungal Agents - chemistry
Bacteriology
Biomedical and Life Sciences
Bioorganic Chemistry
Candida albicans
Fungal infections
Life Sciences
Medicinal Chemistry
Microbial Sensitivity Tests
Microbiology
Natural products
Organic Chemistry
Peptides
Pharmaceutical sciences
Specialty products
Structure-activity relationships
Synthesis
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Summary: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.
ISSN:0021-8820
1881-1469
DOI:10.1038/s41429-023-00700-4