Synthesis and structure-activity relationship studies of novel [6,6,5] tricyclic oxazolidinone derivatives as potential antibacterial agents
文献类型：期刊论文
| 作者 | Xue, Tao1; Ding, Shi1; Guo, Bin1 ; Chu, Wenjing1; Wang, Hui2; Yang, Yushe1
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| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
 |
| 出版日期 | 2015-05-15 |
| 卷号 | 25期号:10页码:2203-2210 |
| 关键词 | [6,6,5] tricyclic core structure Structure-activity relationship Antibacterial activity Liver microsomal stability |
| ISSN号 | 0960-894X |
| DOI | 10.1016/j.bmcl.2015.03.053 |
| 文献子类 | Article |
| 英文摘要 | In our previous Letter, we reported the discovery of a novel benzoxazinyl-oxazolidinone antibacterial candidate 2. In order to identify a potential backup compound, extensive modifications on the B/C ring and C3 side chain were undertaken. A series of novel [6,6,5] tricyclic analogues were synthesized and their in vitro antibacterial activities were tested against a panel of susceptible and resistant Gram-positive pathogens. Among of them, benzothiazinyl-oxazolidinones with acetamide or thioamide as C3 side chains exhibited moderate to good antibacterial activity, such as compounds 54, 58, 59 and 63. In vitro liver microsomal stability was further evaluated and the results manifested that compounds 54 and 58 were both metabolically stable in rat and human liver microsomes. Additionally, insights gained from this investigation should provide directions for the further research of new oxazolidinone antibiotics. (C) 2015 Elsevier Ltd. All rights reserved. |
| WOS关键词 | LINEZOLID-RESISTANT STAPHYLOCOCCUS ; OPTIMIZATION ; ANTIBIOTICS |
| 资助项目 | National Natural Science Foundation of China[81172922] |
| WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000353526300036 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/276527]  |
| 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 | Guo, Bin |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China; 2.China Pharmaceut Univ, Dept Microbiol, Nanjing 210009, Jiangsu, Peoples R China |
| 推荐引用方式 GB/T 7714 | Xue, Tao,Ding, Shi,Guo, Bin,et al. Synthesis and structure-activity relationship studies of novel [6,6,5] tricyclic oxazolidinone derivatives as potential antibacterial agents[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2015,25(10):2203-2210. |
| APA | Xue, Tao,Ding, Shi,Guo, Bin,Chu, Wenjing,Wang, Hui,&Yang, Yushe.(2015).Synthesis and structure-activity relationship studies of novel [6,6,5] tricyclic oxazolidinone derivatives as potential antibacterial agents.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,25(10),2203-2210. |
| MLA | Xue, Tao,et al."Synthesis and structure-activity relationship studies of novel [6,6,5] tricyclic oxazolidinone derivatives as potential antibacterial agents".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 25.10(2015):2203-2210. |
入库方式： OAI收割
来源：上海药物研究所
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