Triazole derivatives: A series of Darapladib analogues as orally active Lp-PLA(2) inhibitors
文献类型：期刊论文
| 作者 | Wang, Kai; Xu, Wenwei; Zhang, Wei; Mo, Mingguang; Wang, Yiping ; Shen, Jianhua
|
| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
 |
| 出版日期 | 2013-05-15 |
| 卷号 | 23期号:10页码:2897-2901 |
| 关键词 | Atherosclerosis Lp-PLA(2) inhibitor Imidazole Triazole |
| ISSN号 | 0960-894X |
| DOI | 10.1016/j.bmcl.2013.03.062 |
| 文献子类 | Article |
| 英文摘要 | This Letter reports our efforts towards the optimization of our previously identified series of imidazole and triazole derivatives that lead to the discovery of a series of orally active Lp-PLA(2) inhibitors in C57 mice. These inhibitors are characterized by the presence of a diamine side chain in the molecules, such as 2c, 2f, and 4a. The introduction of the terminal-end amine succeeded in maintaining the in vitro activities at sub-nanomolar levels. The vivo activities could be greatly affected by variations in the two amines via modulating the metabolic stability and lipophilicity of the compounds. (C) 2013 Elsevier Ltd. All rights reserved. |
| WOS关键词 | PHOSPHOLIPASE A(2) ; ATHEROSCLEROSIS |
| 资助项目 | National Science &Technology Major Project 'Key New Drug Creation and Manufacturing Program'[2012ZX09301001-001] ; National Science &Technology Major Project 'Key New Drug Creation and Manufacturing Program'[2012ZX09103101-008] |
| WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000318750000013 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/277618]  |
| 专题 | 药理学第一研究室 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 药物发现与设计中心 |
| 通讯作者 | Wang, Yiping |
| 作者单位 | Chinese Acad Sci, State Key Lab Drug Res, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Wang, Kai,Xu, Wenwei,Zhang, Wei,et al. Triazole derivatives: A series of Darapladib analogues as orally active Lp-PLA(2) inhibitors[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2013,23(10):2897-2901. |
| APA | Wang, Kai,Xu, Wenwei,Zhang, Wei,Mo, Mingguang,Wang, Yiping,&Shen, Jianhua.(2013).Triazole derivatives: A series of Darapladib analogues as orally active Lp-PLA(2) inhibitors.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,23(10),2897-2901. |
| MLA | Wang, Kai,et al."Triazole derivatives: A series of Darapladib analogues as orally active Lp-PLA(2) inhibitors".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 23.10(2013):2897-2901. |
入库方式： OAI收割
来源：上海药物研究所
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