Discovery of benzhydrylpiperazine derivatives as CB1 receptor inverse agonists via privileged structure-based approach
文献类型：期刊论文
| 作者 | Meng, Tao1 ; Wang, Jue2; Peng, Hongli1; Fang, Guanghua1; Li, Min1; Xiong, Bing1; Xie, Xin2; Zhang, Yongliang1; Wang, Xin1; Shen, Jingkang1
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| 刊名 | EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
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| 出版日期 | 2010-03 |
| 卷号 | 45期号:3页码:1133-1139 |
| 关键词 | Benzhydrylpiperazine Privileged structure Cannabinoid receptor 1(CB1) Anti-obesity |
| ISSN号 | 0223-5234 |
| DOI | 10.1016/j.ejmech.2009.12.018 |
| 文献子类 | Article |
| 英文摘要 | The present study describes the identification via privileged structure-based approach of the benzhydrylpiperazine moiety as a potential scaffold to develop novel CB1 receptor modulators. Efficient structural optimization of the initial four hit compounds led to a high quality lead series, represented by compound 6c. Compound 6c is a highly potent and selective CB1 receptor inverse agonist that is able to reduce body weight in diet-induced obese Sprague-Dawley rats. The preparation of privileged structure-based library, the progression from hit to lead, the structure-activity relationships in the lead series and in vitro and in vivo activity of compound 6c are discussed. (C) 2009 Elsevier Masson SAS. All rights reserved. |
| WOS关键词 | MEDICINAL CHEMISTRY ; ANTAGONISTS ; RIMONABANT ; DRUG ; LIGANDS ; OBESITY ; SYSTEM ; TARGET |
| 资助项目 | National High Technology Research and Development Program of China[2007AA02Z308] ; National Science & Technology Major Project "Key New Drug Creation and Manufacturing Program", China[2009ZX09501-010] ; National Natural Science Foundation of China[30672467] ; National Natural Science Foundation of China[30873162] ; National Natural Science Foundation of China[30623008] ; Shanghai Commission of Science and Technology[08JC1407701] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000275404900035 |
| 出版者 | ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/278964]  |
| 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 国家新药筛选中心 |
| 通讯作者 | Peng, Hongli |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China; 2.Natl Ctr Drug Screening, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Meng, Tao,Wang, Jue,Peng, Hongli,et al. Discovery of benzhydrylpiperazine derivatives as CB1 receptor inverse agonists via privileged structure-based approach[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2010,45(3):1133-1139. |
| APA | Meng, Tao.,Wang, Jue.,Peng, Hongli.,Fang, Guanghua.,Li, Min.,...&Shen, Jingkang.(2010).Discovery of benzhydrylpiperazine derivatives as CB1 receptor inverse agonists via privileged structure-based approach.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,45(3),1133-1139. |
| MLA | Meng, Tao,et al."Discovery of benzhydrylpiperazine derivatives as CB1 receptor inverse agonists via privileged structure-based approach".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 45.3(2010):1133-1139. |
入库方式： OAI收割
来源：上海药物研究所
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