State Key Laboratory of Virology, College of Pharmacy, Laojiashan, Wuhan University, Wuhan 430072, China.
Eur J Med Chem. 2010 Sep;45(9):3636-44. doi: 10.1016/j.ejmech.2010.05.009. Epub 2010 May 12.
A novel series of acylides, 3-O-carbamoyl derivatives of 6,11-di-O-methylerythromycin A, were synthesized and evaluated for their antibacterial activity. These compounds have significant antibacterial activity against gram-positive pathogens, including erythromycin-resistant but methicillin-susceptible Staphylococcus aureus, erythromycin-resistant and methicillin-resistant S. aureus, erythromycin-resistant Streptococcus pneumoniae, and gram-negative pathogens, such as Haemophilus influenzae. Among the derivatives tested, compounds 4p, 4r, 4w, 4x and 4z were found to have potent activity against most susceptible and resistant bacteria. Compound 4p exhibited excellent antibacterial activity in comparison to the others.
合成了一系列新型酰基化物，即 6,11-二-O-甲基红霉素 A 的 3-O-氨甲酰基衍生物，并评估了它们的抗菌活性。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。在所测试的衍生物中，化合物 4p、4r、4w、4x 和 4z 被发现对大多数敏感和耐药菌具有很强的活性。与其他化合物相比，化合物 4p 表现出优异的抗菌活性。
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