Synthesis and Antifungal Activity of Rhodopeptin Analogues. 2. Modification of the West Amino Acid Moiety

Structure−activity relationships of the west amino acid modified analogues of rhodopeptins, novel antifungal tetrapeptide isolated from Rhodococcus species Mer-N1033, have been investigated. Among the analogues synthesized, 2,2-difluoro and 2-hydroxy derivatives retained the antifungal activity with...

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Bibliographic Details
Published in:Organic letters 2000-04, Vol.2 (7), p.977-980
Main Authors: Nakayama, Kiyoshi, Kawato, Haruko C, Inagaki, Hiroaki, Nakajima, Ryohei, Kitamura, Akihiro, Someya, Kazuhiko, Ohta, Toshiharu
Format: Article
Language:English
Subjects:
Amino Acids - chemistry
Antifungal Agents - chemical synthesis
Antifungal Agents - pharmacology
Fungi - drug effects
Microbial Sensitivity Tests
Peptides, Cyclic - chemical synthesis
Peptides, Cyclic - pharmacology
Rhodococcus - chemistry
Structure-Activity Relationship
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Summary:Structure−activity relationships of the west amino acid modified analogues of rhodopeptins, novel antifungal tetrapeptide isolated from Rhodococcus species Mer-N1033, have been investigated. Among the analogues synthesized, 2,2-difluoro and 2-hydroxy derivatives retained the antifungal activity with better physical properties, i.e., solubility or acute toxicity.
ISSN:1523-7060
1523-7052
DOI:10.1021/ol005630k