Design, synthesis, and structure-activity relationship studies of conformationally restricted mutilin 14-carbamates
文献类型：期刊论文
| 作者 | Fu, Liqiang; Liu, Xin; Ling, Chenyu; Cheng, Jianjun; Guo, Xingsheng; He, Huili; Ding, Shi; Yang, Yushe
|
| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
 |
| 出版日期 | 2012-01-15 |
| 卷号 | 22期号:2页码:814-819 |
| ISSN号 | 0960-894X |
| 关键词 | Pleuromutilin Gram-positive bacteria Conformationally restriction |
| DOI | 10.1016/j.bmcl.2011.12.063 |
| 文献子类 | Article |
| 英文摘要 | We report herein the design, synthesis, and structure-activity relationship studies of conformationally restricted mutilin 14-carbamates based on the structure of SB-222734. The antibacterial activities of these newly synthesized compounds were also evaluated and compared with linezolid and retapamulin. Results showed that most of the target compounds exhibit good potency in inhibiting the growth of Gram-positive bacteria including Methicillin-susceptible Staphylococcus aureus MSSA (MIC: 0.0625-2 mu g/mL), Methicillin-resistant S. aureus MRSA (MIC: 0.0625-2 mu g/mL), Methicillin-susceptible Staphylococcus epidermidis MSSE (MIC: 0.0625-2 mu g/mL), Methicillin-resistant S. epidermidis MRSE (MIC: 0.0625-2 mu g/mL), and Streptococcus pneumonia (MIC: 0.0625-4 mu g/mL). In particular, three remarkable compounds of this series (12l, 12m, and 21l) exhibited comparable in vitro antibacterial profiles to that of retapamulin. (C) 2011 Elsevier Ltd. All rights reserved. |
| WOS关键词 | GRAM-POSITIVE PATHOGENS ; ENHANCED ANTIMICROBIAL ACTIVITY ; VIVO ANTIBACTERIAL ACTIVITY ; PLEUROMUTILIN DERIVATIVES ; PART 1 ; INHIBITORS ; ANTIBIOTICS ; SELECTIVITY ; DISCOVERY |
| 资助项目 | Key New Drug Creation and Manufacturing Program, China[2009ZX09301-001] ; National Science and Technology Major Project[00000000] |
| WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| WOS记录号 | WOS:000299653500007 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/278217]  |
| 专题 | 药物化学研究室 中科院受体结构与功能重点实验室 新药研究国家重点实验室 |
| 通讯作者 | Yang, Yushe |
| 作者单位 | Chinese Acad Sci, Shanghai Inst Biol Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Fu, Liqiang,Liu, Xin,Ling, Chenyu,et al. Design, synthesis, and structure-activity relationship studies of conformationally restricted mutilin 14-carbamates[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2012,22(2):814-819. |
| APA | Fu, Liqiang.,Liu, Xin.,Ling, Chenyu.,Cheng, Jianjun.,Guo, Xingsheng.,...&Yang, Yushe.(2012).Design, synthesis, and structure-activity relationship studies of conformationally restricted mutilin 14-carbamates.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,22(2),814-819. |
| MLA | Fu, Liqiang,et al."Design, synthesis, and structure-activity relationship studies of conformationally restricted mutilin 14-carbamates".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 22.2(2012):814-819. |
入库方式： OAI收割
来源：上海药物研究所
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