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 better physical properties, i.e., solubility or acute toxicity.
Nakayama
K
K
New Product Research Laboratories I, Daiichi Pharmaceutical Co. Ltd, Tokyo, Japan.
Kawato
H C
HC
Inagaki
H
H
Nakajima
R
R
Kitamura
A
A
Someya
K
K
Ohta
T
T
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
D000596:Amino Acids; D000935:Antifungal Agents; D010456:Peptides, Cyclic