[Selective modification of the free amino groups of the antibiotic ristomycin A].
Selective chemical modification of ristomycin A (I) by the free NH2 groups was performed. 6 different N-acyl and N-aminoacyl derivatives of I were obtained. 5 of them showed antibacterial activity within 0.4-10.0 micrograms/ml against 4 test microbes. The biological activity of the derivatives depended on the substituent type and the molecule total charge: mono-N-L-isoleucyl-I with the charge of +2 had the highest activity and N,N'-disuccinyl-I had the lowest activity.
D000215:Acylation; D000588:Amines; D000596:Amino Acids / Q000032:analysis; D001419:Bacteria / Q000187:drug effects; D004590:Electrophoresis, Paper; D012310:Ristocetin / Q000032:analysis / Q000138:chemical synthesis* / Q000494:pharmacology; D013055:Spectrophotometry, Infrared; D013056:Spectrophotometry, Ultraviolet; D013329:Structure-Activity Relationship
D000588:Amines; D000596:Amino Acids; D012310:Ristocetin; C016719:ristocetin A
Izbiratel'naia modifikatsiia svobodnykh aminogrupp antibiotika ristomitsina A.