| Synthesis and antibacterial activity of 4“-O-carbamoyl analogs of clarithromycin |
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| 引用本文： | Xue Cui Shen,Bo Jiao,Shu Tao Ma. Synthesis and antibacterial activity of 4“-O-carbamoyl analogs of clarithromycin[J]. 中国化学快报, 2010, 21(3): 257-260. DOI: 10.1016/j.cclet.2009.11.023 |
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| 作者姓名： | Xue Cui Shen Bo Jiao Shu Tao Ma |
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| 作者单位： | School of Pharmaceutical Sciences, Shandong University, Jinan 250012, China |
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| 基金项目： | supported by Major R&D Program of New Drugs—National S&T Key Special Subject of China (No.2009ZX09103-115);;National Natural Science Foundation of China(No.20872081);;Natural Science Foundation of Shandong(No.Y2006C31) |
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| 摘 要： | <正>A series of novel 4"-O-carbamoyl analogs of clarithromycin were synthesized and evaluated for their in vitro antibacterial activity. All of the desired compounds showed excellent activity against erythromycin-susceptible S.pneumoniae.Particularly,4-fluorobenzyl carbamate 7a demonstrated potent activity against erythromycin-resistant S.pneumoniae encoded by the mef gene,and remarkably improved activity against erythromycin-resistant S.pneumoniae encoded by the erm gene,and the erm and mef genes.
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| 收稿时间： | 2009-08-26 |
Synthesis and antibacterial activity of 4'-O-carbamoyl analogs of clarithromycin |
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| Xue Cui Shen,Bo Jiao,Shu Tao Ma. Synthesis and antibacterial activity of 4'-O-carbamoyl analogs of clarithromycin[J]. Chinese Chemical Letters, 2010, 21(3): 257-260. DOI: 10.1016/j.cclet.2009.11.023 |
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| Authors: | Xue Cui Shen Bo Jiao Shu Tao Ma |
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| Affiliation: | School of Pharmaceutical Sciences, Shandong University, Jinan 250012, China |
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| Abstract: | A series of novel 4"-O-carbamoyl analogs of clarithromycin were synthesized and evaluated for their in vitro antibacterial activity. All of the desired compounds showed excellent activity against erythromycin-susceptible S.pneumoniae.Particularly,4-fluorobenzyl carbamate 7a demonstrated potent activity against erythromycin-resistant S.pneumoniae encoded by the mef gene,and remarkably improved activity against erythromycin-resistant S.pneumoniae encoded by the erm gene,and the erm and mef genes. |
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| Keywords: | Clarithromycin analogs 4" -O-carbamate Synthesis Antibacterial activity Resistant bacteria |
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