Synthesis and in vitro antibacterial activity of gemifloxacin derivatives containing a substituted benzyloxime moiety
文献类型：期刊论文
| 作者 | Feng, Lianshun1,2,3,4; Lv, Kai1,2; Liu, Mingliang1,2; Wang, Shuo1,2; Zhao, Jing3; You, Xuefu1,2; Li, Sujie1,2; Cao, Jue1,2; Guo, Huiyuan1,2 |
| 刊名 | EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
 |
| 出版日期 | 2012-09-01 |
| 卷号 | 55页码:125-136 |
| 关键词 | Gemifloxacin Derivatives Synthesis Antibacterial Activity |
| ISSN号 | 0223-5234 |
| DOI | 10.1016/j.ejmech.2012.07.010 |
| 英文摘要 | A series of novel gemifloxacin (GMFX) derivatives containing a substituted benzyloxime moiety with remarkable improvement in lipophilicity were synthesized. The target compounds evaluated for their in vitro antibacterial activity against representative strains. Our results reveal that most of the target compounds have considerable potency against all of the tested Gram-positive strains including MRSA and MRSE (MIC: <0.008-8 mu g/mL), although they are generally less active than the references against the Gram-negative strains. In particular, compound 111 (MIC: <0.008-4 mu g/mL) was found to be 8-2048 and 2-128 times more potent than levofloxacin (LVFX) and GMFX against the Gram-positive strains, respectively. Moreover, against MRSA clinical isolates, 111 (MIC90: 1 mu g/mL) is 8-fold more active than GMFX, and 2-fold more active than GMFX and moxifloxacin against MRSE clinical isolates (MIC90: 4 mu g/mL). Crown Copyright (C) 2012 Published by Elsevier Masson SAS. All rights reserved. |
| 语种 | 英语 |
| WOS记录号 | WOS:000309494100014 |
| 出版者 | ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER |
| 源URL | [http://ir.iccas.ac.cn/handle/121111/49649]  |
| 专题 | 中国科学院化学研究所 |
| 通讯作者 | Liu, Mingliang |
| 作者单位 | 1.Chinese Acad Med Sci, Inst Med Biotechnol, Beijing 100050, Peoples R China 2.Peking Union Med Coll, Beijing 100050, Peoples R China 3.Peking Univ, Shenzhen Grad Sch, Sch Chem Biol & Biotechnol, Nanomicro Mat Res Ctr, Shenzhen 518055, Peoples R China 4.Peking Univ, Coll Chem & Mol Engn, Dept Biol Chem, Beijing Natl Lab Mol Sci, Beijing 100871, Peoples R China |
| 推荐引用方式 GB/T 7714 | Feng, Lianshun,Lv, Kai,Liu, Mingliang,et al. Synthesis and in vitro antibacterial activity of gemifloxacin derivatives containing a substituted benzyloxime moiety[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2012,55:125-136. |
| APA | Feng, Lianshun.,Lv, Kai.,Liu, Mingliang.,Wang, Shuo.,Zhao, Jing.,...&Guo, Huiyuan.(2012).Synthesis and in vitro antibacterial activity of gemifloxacin derivatives containing a substituted benzyloxime moiety.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,55,125-136. |
| MLA | Feng, Lianshun,et al."Synthesis and in vitro antibacterial activity of gemifloxacin derivatives containing a substituted benzyloxime moiety".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 55(2012):125-136. |
入库方式： OAI收割
来源：化学研究所
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