Design, synthesis, and biological evaluation of 2-(phenoxyaryl)-3-urea derivatives as novel P2Y(1) receptor antagonists
文献类型：期刊论文
| 作者 | Peng, Jingjing2,3; Zhao, Lifen2; Wang, Lanlan1; Chen, Hui2,3; Qiu, Yunguang2,3; Wang, Jiang2,3 ; Yang, Huaiyu4; Liu, Jun1; Liu, Hong2,3
|
| 刊名 | EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
 |
| 出版日期 | 2018-10-05 |
| 卷号 | 158页码:302-310 |
| 关键词 | P2Y(1) receptor antagonist 2-(phenoxyaryl)-3-urea derivatives Anti-Platelet |
| ISSN号 | 0223-5234 |
| DOI | 10.1016/j.ejmech.2018.09.014 |
| 文献子类 | Article |
| 英文摘要 | A novel series of 2-(phenoxyaryl)-3-urea derivatives were designed, synthesized, and biologically evaluated for their anti-thrombotic activity. Most of compounds exhibited good inhibition against P2Y(1) receptor. Among them, three compounds 11, 12, and 13 demonstrated good P2Y(1) receptor antagonistic potency in vitro (IC50 = 0.62 mu M, 0.82 mu M, and 0.21 mu M, respectively). In antiplatelet aggregation study, four compounds 2, 3, 9, and 13 showed good antiplatelet activity. The possible binding modes of compounds with P2Y(1) receptor were also explored by molecular docking simulation. The docking studies demonstrated that compound 13 interacted well with Phe119 through hydrophobic interaction and modestly improved the P2Y(1) receptor antagonistic activity, making it justifiable for further investigation. (C) 2018 Published by Elsevier Masson SAS. |
| WOS关键词 | PLATELET-AGGREGATION ; ANTIPLATELET AGENTS ; HIGH-AFFINITY ; DIARYL UREAS ; THROMBOSIS ; DISCOVERY ; POTENT ; MICE ; PHARMACOKINETICS ; CLOPIDOGREL |
| 资助项目 | National Natural Science Foundation of China[81620108027] ; National Natural Science Foundation of China[21632008] ; National Natural Science Foundation of China[21672231] ; National Natural Science Foundation of China[21472209] ; Major Project of Chinese National Programs for Fundamental Research and Development[2015CB910304] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000448094000022 |
| 出版者 | ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/279537]  |
| 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 | Liu, Jun; Liu, Hong |
| 作者单位 | 1.China Pharmaceut Univ, Jiangsu Key Lab Drug Screening, Nanjing 210009, Jiangsu, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, 555 Zu Chong Zhi Rd, Shanghai 201203, Peoples R China; 3.Univ Chinese Acad Sci, 19A Yuquan Rd, Beijing 100049, Peoples R China; 4.East China Normal Univ, Sch Life Sci, Inst Biomed Sci, Shanghai Key Lab Regulatory Biol, Shanghai 200241, Peoples R China |
| 推荐引用方式 GB/T 7714 | Peng, Jingjing,Zhao, Lifen,Wang, Lanlan,et al. Design, synthesis, and biological evaluation of 2-(phenoxyaryl)-3-urea derivatives as novel P2Y(1) receptor antagonists[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2018,158:302-310. |
| APA | Peng, Jingjing.,Zhao, Lifen.,Wang, Lanlan.,Chen, Hui.,Qiu, Yunguang.,...&Liu, Hong.(2018).Design, synthesis, and biological evaluation of 2-(phenoxyaryl)-3-urea derivatives as novel P2Y(1) receptor antagonists.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,158,302-310. |
| MLA | Peng, Jingjing,et al."Design, synthesis, and biological evaluation of 2-(phenoxyaryl)-3-urea derivatives as novel P2Y(1) receptor antagonists".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 158(2018):302-310. |
入库方式： OAI收割
来源：上海药物研究所
浏览0
下载0
收藏0
其他版本
除非特别说明，本系统中所有内容都受版权保护，并保留所有权利。