Discovery of 2-Alkyl-1-arylsulfonylprolinamides as 11 beta-Hydroxysteroid Dehydrogenase Type 1 Inhibitors
文献类型：期刊论文
| 作者 | Yu, Jianxin2; Liu, Haiyan2; Xia, Guangxin1,2; Liu, Lin1,2; Xu, Zhenmin2; Chen, Qian2; Ma, Chen2; Sun, Xing2; Xu, Jiajun2; Li, Hua2 |
| 刊名 | ACS MEDICINAL CHEMISTRY LETTERS
 |
| 出版日期 | 2012-10 |
| 卷号 | 3期号:10页码:793-798 |
| 关键词 | metabolic syndrome enzyme inhibitor 11 beta-hydroxysteroid dehydrogenase type 1 sulfonamide 2-alkylproline prolinamide |
| ISSN号 | 1948-5875 |
| DOI | 10.1021/ml300144n |
| 文献子类 | Article |
| 英文摘要 | On the basis of scaffold hopping, a novel series of 2-alkyl-1-arylsulfonylprolinamides was discovered as 11 beta-hydroxysteroid dehydrogenase type 1 (11 beta-HSD-1) inhibitors. A representative compound 4ek, obtained through SAR and structure optimization studies, demonstrates excellent in vitro potency against 11 beta-HSD-1 and dose-dependent in vivo inhibition of 11 beta-HSD-1 in a prednisone/prednisolone transformation biomarker study in mice. |
| WOS关键词 | SELECTIVE INHIBITORS ; 11-BETA-HSD1 INHIBITORS ; BIOLOGICAL EVALUATION ; METABOLIC SYNDROME ; POTENT ; PHARMACOKINETICS ; MICE |
| 资助项目 | New Drug Creation Project of the National Science and Technology Major Foundation of China[2010ZX09401-404] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000309649100008 |
| 出版者 | AMER CHEMICAL SOC |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/277918]  |
| 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 | Xia, Guangxin |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China 2.Shanghai Pharmaceut Holding Co Ltd, Cent Res Inst, Shanghai 201203, Peoples R China; |
| 推荐引用方式 GB/T 7714 | Yu, Jianxin,Liu, Haiyan,Xia, Guangxin,et al. Discovery of 2-Alkyl-1-arylsulfonylprolinamides as 11 beta-Hydroxysteroid Dehydrogenase Type 1 Inhibitors[J]. ACS MEDICINAL CHEMISTRY LETTERS,2012,3(10):793-798. |
| APA | Yu, Jianxin.,Liu, Haiyan.,Xia, Guangxin.,Liu, Lin.,Xu, Zhenmin.,...&Shen, Jingkang.(2012).Discovery of 2-Alkyl-1-arylsulfonylprolinamides as 11 beta-Hydroxysteroid Dehydrogenase Type 1 Inhibitors.ACS MEDICINAL CHEMISTRY LETTERS,3(10),793-798. |
| MLA | Yu, Jianxin,et al."Discovery of 2-Alkyl-1-arylsulfonylprolinamides as 11 beta-Hydroxysteroid Dehydrogenase Type 1 Inhibitors".ACS MEDICINAL CHEMISTRY LETTERS 3.10(2012):793-798. |
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。