A novel polycationic analogue of gratisin with antibiotic activity against both Gram-positive and Gram-negative bacteria.
A novel polycationic analogue of gratisin, cyclo(-Val-Orn-Leu-D-Phe-Pro-D-Lys-)2, was designed and synthesized, which exhibited strong activity against all Gram-positive and Gram-negative bacteria tested. Its activity against Pseudomonas aeruginosa IFO 3080 was two times higher than gramicidin S.
Tamaki
Makoto
M
Department of Chemistry, Toho University, Funabashi, Chiba, Japan. tamaki@chem.sci.toho-u.ac.jp
Kokuno
Manabu
M
Suzuki
Yumiko
Y
Iwama
Mitsuko
M
Shindo
Mitsuno
M
Uchida
Yoshiki
Y
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D023181:Antimicrobial Cationic Peptides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D002942:Circular Dichroism; D015195:Drug Design; D006090:Gram-Negative Bacteria / Q000187:drug effects*; D006094:Gram-Positive Bacteria / Q000187:drug effects*; D008826:Microbial Sensitivity Tests; D010455:Peptides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D010456:Peptides, Cyclic / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D011550:Pseudomonas aeruginosa / Q000187:drug effects
D000900:Anti-Bacterial Agents; D023181:Antimicrobial Cationic Peptides; D010455:Peptides; D010456:Peptides, Cyclic; C529284:cyclo(valyl-ornithyl-leucyl-phenylalanyl-prolyl-lysyl)2; C033282:gratisin