Design, synthesis, and biological evaluation of novel 2-methylpiperazine derivatives as potent CCR5 antagonists
文献类型：期刊论文
| 作者 | Hu, Suwen1; Wang, Zhilong2; Hou, Tingjun1,3; Ma, Xiaodong1; Li, Jing2 ; Liu, Tao1; Xie, Xin2; Hu, Yongzhou1
|
| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY
 |
| 出版日期 | 2015-03-01 |
| 卷号 | 23期号:5页码:1157-1168 |
| 关键词 | CCR5 antagonist Anti-HIV-1 agent 2-Methylpiperazine derivatives |
| ISSN号 | 0968-0896 |
| DOI | 10.1016/j.bmc.2014.12.052 |
| 文献子类 | Article |
| 英文摘要 | Three series of novel 2-methylpiperazine derivatives were designed and synthesized using a fragment-assembly strategy. Among them, six compounds (13, 16, 18, 22, 33, and 36) showed potent activity against CCR5 comparable to that of the positive control, maraviroc, in calcium mobilization assay. Moreover, some compounds were selected and further tested for their antiviral activity in HIV-1 single cycle assay. As a result, four compounds (13, 16, 33, and 36) showed antiviral activity at the nanomolar level. Additionally, the potent four compounds showed no cytotoxicity at a concentration of 10 mu M. (C) 2015 Elsevier Ltd. All rights reserved. |
| WOS关键词 | HIV-INFECTION ; INHIBITORS |
| 资助项目 | National Natural Science Foundation of China[81072515] ; National Natural Science Foundation of China[81202341] ; Ministry of Health-medical Science Critical Technological Program of Zhejiang Province[WKJ20122024] ; Program for Zhejiang Leading Team of ST Innovation[2011R50014] ; National Basic Research Program of China (973 Program)[2014CB541906] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000349966700024 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/276627]  |
| 专题 | 国家新药筛选中心 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 药物化学研究室 |
| 通讯作者 | Liu, Tao |
| 作者单位 | 1.Zhejiang Univ, Coll Pharmaceut Sci, ZJU ENS Joint Lab Med Chem, Hangzhou 310058, Zhejiang, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, Natl Ctr Drug Screening, State Key Lab Drug Res, Shanghai 201203, Peoples R China; 3.Soochow Univ, Inst Funct Nano & Soft Mat FUNSOM, Suzhou 215123, Jiangsu, Peoples R China |
| 推荐引用方式 GB/T 7714 | Hu, Suwen,Wang, Zhilong,Hou, Tingjun,et al. Design, synthesis, and biological evaluation of novel 2-methylpiperazine derivatives as potent CCR5 antagonists[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2015,23(5):1157-1168. |
| APA | Hu, Suwen.,Wang, Zhilong.,Hou, Tingjun.,Ma, Xiaodong.,Li, Jing.,...&Hu, Yongzhou.(2015).Design, synthesis, and biological evaluation of novel 2-methylpiperazine derivatives as potent CCR5 antagonists.BIOORGANIC & MEDICINAL CHEMISTRY,23(5),1157-1168. |
| MLA | Hu, Suwen,et al."Design, synthesis, and biological evaluation of novel 2-methylpiperazine derivatives as potent CCR5 antagonists".BIOORGANIC & MEDICINAL CHEMISTRY 23.5(2015):1157-1168. |
入库方式： OAI收割
来源：上海药物研究所
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