Efficient synthesis and identification of novel propane-1,3-diamino bridged CCR5 antagonists with variation on the basic center carrier
文献类型：期刊论文
| 作者 | Fan, Xing1; Zhang, Hu-Shan1; Chen, Li2; Long, Ya-Qiu1 |
| 刊名 | EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
 |
| 出版日期 | 2010-07 |
| 卷号 | 45期号:7页码:2827-2840 |
| 关键词 | CCR5 antagonist Propane-1,3-diamine Convergent synthesis (S)-beta-amino-beta-arylpropanal 4-Amino-4-methylpiperidine Basic center carrier |
| ISSN号 | 0223-5234 |
| DOI | 10.1016/j.ejmech.2010.03.003 |
| 文献子类 | Article |
| 英文摘要 | By employing pharmacophore-based design and the privileged fragments reassembly, a series of piperidine-/tropane-/piperazine-bridged CCR5 antagonists were designed and synthesized via an efficient convergent synthesis strategy, with focus on the optimal choice of the basic center carrier structure. Significantly, the 4-amino-4-methylpiperidine bridged 1-acyl-1,3-propanediamine compounds were identified as a new class of nanomolar CCR5 antagonists, providing an efficient approach and novel scaffolds for further development of potent CCR5 inhibitors. (C) 2010 Elsevier Masson SAS. All rights reserved. |
| WOS关键词 | SMALL-MOLECULE CCR5 ; BETA-AMINO ; REDUCTIVE AMINATION ; HIV-1 INHIBITORS ; DISCOVERY ; RECEPTOR ; POTENT ; DERIVATIVES ; HETEROCYCLES ; EPIBATIDINE |
| 资助项目 | National Natural Science Foundation of China[30672528] ; Science and Technology Commission of Shanghai Municipality[07QH14018] ; Science and Technology Commission of Shanghai Municipality[08JC1422200] ; National Science and Technology Major Project[2009ZX09301-001] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000278626400016 |
| 出版者 | ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/278855]  |
| 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 | Long, Ya-Qiu |
| 作者单位 | 1.CAS, Shanghai Inst Biol Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China; 2.Shanghai TargetDrug Co Ltd, Shanghai 200233, Peoples R China |
| 推荐引用方式 GB/T 7714 | Fan, Xing,Zhang, Hu-Shan,Chen, Li,et al. Efficient synthesis and identification of novel propane-1,3-diamino bridged CCR5 antagonists with variation on the basic center carrier[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2010,45(7):2827-2840. |
| APA | Fan, Xing,Zhang, Hu-Shan,Chen, Li,&Long, Ya-Qiu.(2010).Efficient synthesis and identification of novel propane-1,3-diamino bridged CCR5 antagonists with variation on the basic center carrier.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,45(7),2827-2840. |
| MLA | Fan, Xing,et al."Efficient synthesis and identification of novel propane-1,3-diamino bridged CCR5 antagonists with variation on the basic center carrier".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 45.7(2010):2827-2840. |
入库方式： OAI收割
来源：上海药物研究所
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