Design and synthesis of imidazole and triazole derivatives as Lp-PLA(2) inhibitors and the unexpected discovery of highly potent quaternary ammonium salts
文献类型：期刊论文
| 作者 | Wang, Kai; Xu, Wenwei; Liu, Yang; Zhang, Wei; Wang, Wenyi; Shen, Jianhua ; Wang, Yiping
|
| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
 |
| 出版日期 | 2013-03-01 |
| 卷号 | 23期号:5页码:1187-1192 |
| 关键词 | Bioisosteric replacement Imidazole Triazole Lp-PLA(2) inhibitor Quaternary ammonium salt |
| ISSN号 | 0960-894X |
| DOI | 10.1016/j.bmcl.2013.01.029 |
| 文献子类 | Article |
| 英文摘要 | New Lp-PLA2 inhibitors were synthesized by the bioisosteric replacement of the amide group of Darapladib with an imidazole or a triazole. Unfortunately, the inhibitory activities of these derivatives were lower than that of Darapladib. But interestingly, a series of quaternary ammonium salts that were isolated as by-products during this synthetic work were found with high potency. Of these by-products, compound 22c showed a similar profile to Darapladib both in vitro and in vivo. (C) 2013 Elsevier Ltd. All rights reserved. |
| WOS关键词 | CORONARY-ARTERY-DISEASE ; PHOSPHOLIPASE A(2) ; HEART-DISEASE ; LIPOPROTEIN ; ATHEROSCLEROSIS ; RISK ; MECHANISMS ; EVENTS |
| 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:000314693400005 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/277717]  |
| 专题 | 药物发现与设计中心 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 药理学第一研究室 |
| 通讯作者 | Shen, Jianhua |
| 作者单位 | Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Wang, Kai,Xu, Wenwei,Liu, Yang,et al. Design and synthesis of imidazole and triazole derivatives as Lp-PLA(2) inhibitors and the unexpected discovery of highly potent quaternary ammonium salts[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2013,23(5):1187-1192. |
| APA | Wang, Kai.,Xu, Wenwei.,Liu, Yang.,Zhang, Wei.,Wang, Wenyi.,...&Wang, Yiping.(2013).Design and synthesis of imidazole and triazole derivatives as Lp-PLA(2) inhibitors and the unexpected discovery of highly potent quaternary ammonium salts.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,23(5),1187-1192. |
| MLA | Wang, Kai,et al."Design and synthesis of imidazole and triazole derivatives as Lp-PLA(2) inhibitors and the unexpected discovery of highly potent quaternary ammonium salts".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 23.5(2013):1187-1192. |
入库方式： OAI收割
来源：上海药物研究所
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