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糖肽类抗生素A-40926及其苷元衍生物的合成与抗菌活性

Synthesis and antibacterial activity of derivatives of the glycopeptide antibiotic A-40926 and its aglycone.

作者信息

Hermann R, Ripamonti F, Romanò G, Restelli E, Ferrari P, Goldstein B P, Berti M, Ciabatti R

机构信息

Lepetit Research Center, Gerenzano (Varese), Italy.

出版信息

J Antibiot (Tokyo). 1996 Dec;49(12):1236-48. doi: 10.7164/antibiotics.49.1236.

DOI:10.7164/antibiotics.49.1236
PMID:9031670
Abstract

Starting from the antibiotic A-40926 and the aglycone of A-40926 a series of compounds were prepared by modifying the free functionalities. Their antimicrobial activity was determined, particularly against Neisseria gonorrhoeae, against which A-40926, unlike other natural glycopeptides, is active. Improved in vivo activity was displayed by the monomethyl ester of A-40926 esterified at the carboxyl group of the N-acylamino-glucuronyl moiety.

摘要

从抗生素A - 40926及其苷元出发,通过修饰游离官能团制备了一系列化合物。测定了它们的抗菌活性,特别是针对淋病奈瑟菌的活性,与其他天然糖肽不同,A - 40926对其具有活性。在N - 酰基氨基葡萄糖醛酸部分的羧基处酯化的A - 40926单甲酯表现出改善的体内活性。

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