螺旋霉素的化学修饰。IV. 螺旋霉素I的3'',4''-二酰化物和3,3'',4''-三酰化物的合成及其体外和体内活性
Chemical modification of spiramycins. IV. Synthesis and in vitro and in vivo activities of 3'',4''-diacylates and 3,3'',4''-triacylates of spriamycin I.
作者信息
Sano H, Sunazuka T, Tanaka H, Yamashita K, Okachi R, Omura S
出版信息
J Antibiot (Tokyo). 1984 Jul;37(7):760-72. doi: 10.7164/antibiotics.37.760.
PMID:6469870
Abstract
3'',4''-Diacylates and 3,3'',4''-triacylates of spiramycin I were synthesized and evaluated by the four parameters, MIC against bacteria, affinity to ribosomes, retention time in HPLC and therapeutic effect. Among them, 3,3'',4''-tri-O-propionyl and 3,4''-di-O-acetyl-3''-O-butyryl-spiramycin I were the most active in vivo, which were superior to acetylspiramycin.
摘要
合成了螺旋霉素I的3'',4''-二酰化物和3,3'',4''-三酰化物，并通过四个参数进行评估，即对细菌的最低抑菌浓度（MIC）、对核糖体的亲和力、在高效液相色谱（HPLC）中的保留时间和治疗效果。其中，3,3'',4''-三-O-丙酰基螺旋霉素I和3,4''-二-O-乙酰基-3''-O-丁酰基螺旋霉素I在体内活性最高，优于乙酰螺旋霉素。
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