A novel active analogue of gramicidin S with smaller ring size.
A novel active gramicidin S analogue with smaller ring size, cyclo[-delta-Orn(-Val-Pro-D-Phe-H)-Leu-]2, was synthesized and examined the structure-activity relationship. Its analogue showed antibiotic activity against all Gram-positive microorganisms tested, and its activity was 1/2-1/8 of that of gramicidin S. The present results indicated that both structures of cyclo(-delta-Orn-Leu-)2 and H-D-Phe-Pro-Val sequence play the important role for showing the antibiotic activity.
Makoto
M
Tamaki
Rie
R
Ishii
Sho
S
Kikuchi
Eiji
E
Watanabe
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D001419:Bacteria / Q000187:drug effects; D003500:Cyclization; D006096:Gramicidin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry*; D009682:Magnetic Resonance Spectroscopy; D008826:Microbial Sensitivity Tests; D013329:Structure-Activity Relationship
D000900:Anti-Bacterial Agents; D006096:Gramicidin