4-(Phenylsulfonamidomethyl) benzamides as potent and selective inhibitors of the 11 beta-hydroxysteroid dehydrogenase type 1 with efficacy in diabetic ob/ob mice
文献类型：期刊论文
| 作者 | Zhang, Xu; Zhou, Zhou; Yang, Huaiyu; Chen, Junhua; Feng, Ying; Du, Lili; Leng, Ying ; Shen, Jianhua
|
| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
 |
| 出版日期 | 2009-08-01 |
| 卷号 | 19期号:15页码:4455-4458 |
| 关键词 | 11 beta-HSD1 inhibitors 4-(Phenylsulfonamidomethyl) benzamide Type 2 diabetes |
| ISSN号 | 0960-894X |
| DOI | 10.1016/j.bmcl.2009.05.033 |
| 文献子类 | Article |
| 英文摘要 | Selective inhibitors of 11 beta-hydroxysteroid dehydrogenase type 1 (11 beta-HSD1) have considerable potential as treatments for type 2 diabetes. Presented herein are the syntheses, structure-activity relationships, and efficacy evaluation of 4-(phenylsulfonamidomethyl) benzamides as 11 beta-HSD1 inhibitors. Through modi. cation of our initial lead 5, we have identified potent and selective 11 beta-HSD1 inhibitors, such as 11n, which demonstrated improved glycemic control, decreased serum lipids, and enhanced insulin sensitivity when dosed ip in diabetic ob/ob mice. Crown Copyright (C) 2009 Published by Elsevier Ltd. All rights reserved. |
| WOS关键词 | METABOLIC SYNDROME ; VISCERAL OBESITY |
| 资助项目 | National Basic Research Program of China[2009CB522300] ; 863 Hi-Tech Program of China[2006AA020602] ; National Natural Science Foundation of China[90813029] ; Science and Technology Commission of Shanghai Municipality[08ZR1422600] |
| WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000267900900101 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/279170]  |
| 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, Xu,Zhou, Zhou,Yang, Huaiyu,et al. 4-(Phenylsulfonamidomethyl) benzamides as potent and selective inhibitors of the 11 beta-hydroxysteroid dehydrogenase type 1 with efficacy in diabetic ob/ob mice[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2009,19(15):4455-4458. |
| APA | Zhang, Xu.,Zhou, Zhou.,Yang, Huaiyu.,Chen, Junhua.,Feng, Ying.,...&Shen, Jianhua.(2009).4-(Phenylsulfonamidomethyl) benzamides as potent and selective inhibitors of the 11 beta-hydroxysteroid dehydrogenase type 1 with efficacy in diabetic ob/ob mice.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,19(15),4455-4458. |
| MLA | Zhang, Xu,et al."4-(Phenylsulfonamidomethyl) benzamides as potent and selective inhibitors of the 11 beta-hydroxysteroid dehydrogenase type 1 with efficacy in diabetic ob/ob mice".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 19.15(2009):4455-4458. |
入库方式： OAI收割
来源：上海药物研究所
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