新型 6,11-二-O-甲基红霉素 A 的 4''-氨基甲酸酯的合成与抗菌活性。

Synthesis and antibacterial activity of novel 4''-carbamates of 6,11-di-O-methylerythromycin A.

机构信息

College of Pharmacy, Wuhan University, Wuhan, China.

出版信息

J Antibiot (Tokyo). 2010 Jul;63(7):343-50. doi: 10.1038/ja.2010.44. Epub 2010 May 7.

DOI:10.1038/ja.2010.44

PMID:20448668

Abstract

A novel series of 4''-carbamates of 6,11-di-O-methylerythromycin A were synthesized and evaluated. These compounds have significant antibacterial activity against Gram-positive pathogens, including erythromycin-resistant but methicillin-susceptible Staphylococcus aureus, erythromycin-resistant and methicillin-resistant Staphylococcus aureus, erythromycin-resistant Streptococcus pneumoniae and Gram-negative pathogens, such as Haemophilus influenzae To our surprise, most of the derivatives tested had potent activity against most resistant bacteria. Among these, compounds 10u, 10v, 10w and 10y were found to have potent activity against most susceptible and resistant bacteria. In particular, compound 10y exhibited excellent antibacterial activity in comparison to others.

摘要

我们合成了一系列新型的 6,11-二-O-甲基红霉素 A 的 4''- 氨基甲酸酯，并对其进行了评估。这些化合物对革兰氏阳性病原体具有显著的抗菌活性，包括耐红霉素但对甲氧西林敏感的金黄色葡萄球菌、耐红霉素和耐甲氧西林的金黄色葡萄球菌、耐红霉素的肺炎链球菌以及革兰氏阴性病原体，如流感嗜血杆菌。令我们惊讶的是，大多数测试的衍生物对大多数耐药菌都具有很强的活性。在这些衍生物中，化合物 10u、10v、10w 和 10y 被发现对大多数敏感菌和耐药菌都具有很强的活性。特别是，化合物 10y 的抗菌活性明显优于其他化合物。