Synthesis and evaluation of piperidine urea derivatives as efficacious 11 beta-hydroxysteroid dehydrogenase type 1 inhibitors in diabetic ob/ob mice
文献类型：期刊论文
| 作者 | Zhang, Liming; Chen, Junhua; Ning, Mengmeng ; Zou, Qingan; Leng, Ying; Shen, Jianhua
|
| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
 |
| 出版日期 | 2012-04-15 |
| 卷号 | 22期号:8页码:2748-2752 |
| 关键词 | 11 beta-HSD1 inhibitor Diabetes Metabolic syndrome Amide Urea |
| ISSN号 | 0960-894X |
| DOI | 10.1016/j.bmcl.2012.02.095 |
| 文献子类 | Article |
| 英文摘要 | 11 beta-Hydroxysteroid dehydrogenase type 1 (11 beta-HSD1) has attracted considerable attention as a potential target for the treatment of diabetes and metabolic syndrome. Herein we report the design, synthesis and efficacy evaluation of novel amide and urea 11 beta-HSD1 inhibitors. Structure-activity relationship studies led to the identification of 10c, which was efficacious in a diabetic ob/ob mouse model and reduced fasting and non-fasting blood glucose levels after ip dosing. (C) 2012 Elsevier Ltd. All rights reserved. |
| WOS关键词 | BETA-HYDROXYSTEROID DEHYDROGENASE ; SELECTIVE INHIBITORS ; METABOLIC SYNDROME ; MINERALOCORTICOID ACTION ; OBESITY ; POTENT ; HYPERGLYCEMIA ; 11-BETA-HSD1 ; DETERMINANT ; DISCOVERY |
| 资助项目 | National Natural Science Foundation of China[30901838] |
| WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000302768200021 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/278117]  |
| 专题 | 药理学第一研究室 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 药物发现与设计中心 |
| 通讯作者 | Leng, Ying |
| 作者单位 | Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Zhang, Liming,Chen, Junhua,Ning, Mengmeng,et al. Synthesis and evaluation of piperidine urea derivatives as efficacious 11 beta-hydroxysteroid dehydrogenase type 1 inhibitors in diabetic ob/ob mice[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2012,22(8):2748-2752. |
| APA | Zhang, Liming,Chen, Junhua,Ning, Mengmeng,Zou, Qingan,Leng, Ying,&Shen, Jianhua.(2012).Synthesis and evaluation of piperidine urea derivatives as efficacious 11 beta-hydroxysteroid dehydrogenase type 1 inhibitors in diabetic ob/ob mice.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,22(8),2748-2752. |
| MLA | Zhang, Liming,et al."Synthesis and evaluation of piperidine urea derivatives as efficacious 11 beta-hydroxysteroid dehydrogenase type 1 inhibitors in diabetic ob/ob mice".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 22.8(2012):2748-2752. |
入库方式： OAI收割
来源：上海药物研究所
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