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Synthesis and antifungal activity of rhodopeptin analogues. 2. Modification of the west amino acid moiety
Authors:Nakayama K  Kawato H C  Inagaki H  Nakajima R  Kitamura A  Someya K  Ohta T
Affiliation:New Product Research Laboratories I, Daiichi Pharmaceutical Co. Ltd, Tokyo, Japan.
Abstract: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.
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