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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.

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。

相似文献

1
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.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
J Antibiot (Tokyo). 1984 Jul;37(7):760-72. doi: 10.7164/antibiotics.37.760.
2
Structure activity relationships of spiramycins.螺旋霉素的构效关系
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Chemical modification of spiramycins. III. Synthesis and antibacterial activities of 4''-sulfonates and 4''-alkylethers of spiramycin I.螺旋霉素的化学修饰。III. 螺旋霉素I的4''-磺酸盐和4''-烷基醚的合成及抗菌活性
J Antibiot (Tokyo). 1984 Jul;37(7):750-9. doi: 10.7164/antibiotics.37.750.
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Chemical modification of spiramycins. V. Synthesis and antibacterial activity of 3'- or 4''-de-N-methylspiramycin I and their N-substituted derivatives.螺旋霉素的化学修饰。V. 3'-或4''-去-N-甲基螺旋霉素I及其N-取代衍生物的合成与抗菌活性
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J Med Chem. 1977 May;20(5):732-6. doi: 10.1021/jm00215a025.
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[Spiramycin derivatives. 1].[螺旋霉素衍生物。1]
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