[抗生素瑞斯托菌素A游离氨基的选择性修饰]
[Selective modification of the free amino groups of the antibiotic ristomycin A].
作者信息
Katrukha G S, Smirnova I G, Trifonova Zh P, Smeianova G I
出版信息
Antibiot Med Biotekhnol. 1986 Aug;31(8):588-92.
PMID:3767335
Abstract
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.
摘要
对瑞斯托菌素A（I）的游离氨基进行了选择性化学修饰。得到了I的6种不同的N-酰基和N-氨基酰基衍生物。其中5种在0.4 - 10.0微克/毫升浓度范围内对4种测试微生物表现出抗菌活性。衍生物的生物活性取决于取代基类型和分子总电荷：带 +2电荷的单-N-L-异亮氨酰-I活性最高，而N,N'-二琥珀酰-I活性最低。
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