title: Synthesis and antifungal activity of rhodopeptin analogues. 1. Modification of the east and south amino acid moieties.
abstract: Structure-activity relationships of the east and south amino acid modified analogues of rhodopeptins, novel antifungal cyclic tetrapeptides isolated from Rhodococcus species Mer-N1033, have been investigated. It was observed that a basic amino acid moiety (lysine or ornithine) as the east amino acid and a hydrophobic and bulky neutral amino acid (i.e., gamma-methylleucine) as the south amino acid were indispensable structure motifs for antifungal activity of rhodopeptin analogues.
authors.affiliation: New Product Research Laboratories I, Daiichi Pharmaceutical Co., Ltd., Tokyo, Japan. kawatlm8@daiichipharm.co.jp
authors.forename: H C
authors.initials: HC
authors.lastname: Kawato
authors.forename: K
authors.initials: K
authors.lastname: Nakayama
authors.forename: H
authors.initials: H
authors.lastname: Inagaki
authors.forename: R
authors.initials: R
authors.lastname: Nakajima
authors.forename: A
authors.initials: A
authors.lastname: Kitamura
authors.forename: K
authors.initials: K
authors.lastname: Someya
authors.forename: T
authors.initials: T
authors.lastname: Ohta
mesh_terms: D000596:Amino Acids / Q000737:chemistry*; D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D005658:Fungi / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D010456:Peptides, Cyclic / Q000138:chemical synthesis* / Q000494:pharmacology; D012240:Rhodococcus / Q000737:chemistry; D013329:Structure-Activity Relationship
chemical_list: D000596:Amino Acids; D000935:Antifungal Agents; D010456:Peptides, Cyclic; C401441:rhodopeptin B5