Omura S, Nakagawa A, Sakakibara H, Okekawa O, Brandsch R
J Med Chem. 1977 May;20(5):732-6. doi: 10.1021/jm00215a025.
The synthesis, antimicrobial activity, and binding to ribosomes of leucomycin and leucomycin derivatives are described. In general, the binding of the leucomycins and the leucomycin derivatives to ribosomes correlated with their antimicrobial activity. Some 2'-O-acyl derivatives apparently underwent gradual hydrolysis during antimicrobial assays, for their binding to ribosomes was poor compared to their relatively good antimicrobial activies. Correlation between antimicrobial activity and binding to ribosomes, their molecular site of action, provides some insight into the nature of the active molecular moieties.
描述了柱晶白霉素及其衍生物的合成、抗菌活性以及与核糖体的结合情况。一般来说，柱晶白霉素及其衍生物与核糖体的结合与其抗菌活性相关。一些2'-O-酰基衍生物在抗菌试验中显然会逐渐水解，因为与它们相对较好的抗菌活性相比，它们与核糖体的结合较差。抗菌活性与与核糖体的结合及其分子作用位点之间的相关性，为活性分子部分的性质提供了一些见解。
