Synthesis and antibacterial activity of 4",11-di-O-arylalkylcarbamoyl azithromycin derivatives

被引:21
作者
Ma, Shutao [1 ]
Jiao, Bo [1 ]
Liu, Zhaopeng [1 ]
Wang, Hui [2 ]
Xian, Ruiqing [1 ]
Zheng, Manjie [1 ]
Lou, Hongxiang [1 ]
机构
[1] Shandong Univ, Sch Pharmaceut Sci, Dept Med Chem, Jinan 250012, Peoples R China
[2] Beijing Union Med Coll Hosp, Dept Clin Lab, Beijing 100730, Peoples R China
基金
中国国家自然科学基金;
关键词
4; 11-Disubstituted azithromycin; Synthesis; Antibacterial activity; Macrolide resistance; KETOLIDES;
D O I
10.1016/j.bmcl.2009.01.092
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of new 4 '',11-di-O-arylalkylcarbamoyl azithromycin derivatives were designed, synthesized and evaluated for their in vitro antibacterial activities. Some derivatives exhibited greatly improved activity against erythromycin-resistant bacteria. Among them, compounds 5f and 5k were found to have potent activity against erythromycin-resistant Streptococcus pneumoniae whose resistance was encoded by the erm or mef gene. (C) 2009 Elsevier Ltd. All rights reserved.
引用
收藏
页码:1698 / 1701
页数:4
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