Synthesis and antibacterial activity of new 4"-O-carbamates of 11,12-cyclic carbonate erythromycin A 6,9-imino ether

被引：12

作者：

Zhang, Ling ^{[1
]}

Jiao, Bo ^{[1
]}

Yang, Xiangrui ^{[1
]}

Liu, Lin ^{[1
]}

Ma, Shutao ^{[1
]}

机构：

[1] Shandong Univ, Dept Med Chem, Sch Pharmaceut Sci, Jinan 250012, Peoples R China

来源：

JOURNAL OF ANTIBIOTICS | 2011年 / 64卷 / 03期

基金：

中国国家自然科学基金;

关键词：

antibacterial activity; 4 ''-O-carbamate derivatives; erythromycin A 6,9-imino ether; resistance; synthesis; RIBOSOMAL-RNA; MACROLIDE; RESISTANCE; AZITHROMYCIN; KETOLIDES;

D O I：

10.1038/ja.2010.166

中图分类号：

Q81 [生物工程学（生物技术）]; Q93 [微生物学];

学科分类号：

071005 ; 0836 ; 090102 ; 100705 ;

摘要：

A series of new 4 ''-O-carbamates of 11,12-cyclic carbonate erythromycin A 6,9-imino ether were synthesized and evaluated for their in vitro antibacterial activity. All the desired compounds demonstrated favorable activity (0.03 mu g ml(-1)) against erythromycin-susceptible Streptococcus pneumoniae comparable to the references, exhibiting 133-fold higher activity than precursor 2 or 3. Similarly, all of the analogs exhibited improved activity against the erythromycin-resistant S. pneumoniae encoded by the erm gene and the erm and mef genes, showing 4-32-fold more effectiveness than erythromycin A. The Journal of Antibiotics (2011) 64, 243-247; doi:10.1038/ja.2010.166; published online 19 January 2011

引用

页码：243 / 247

页数：5

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