Derivatives of (phenylsulfonamido-methyl)nicotine and (phenylsulfonamido-methyl)thiazole as novel 11 beta-hydroxysteroid dehydrogenase type 1 inhibitors: synthesis and biological activities in vitro
文献类型：期刊论文
| 作者 | Zhang, Xu; Zhou, Yang; Shen, Yu; Du, Li-li; Chen, Jun-hua; Leng, Ying ; Shen, Jian-hua
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| 刊名 | ACTA PHARMACOLOGICA SINICA
 |
| 出版日期 | 2009-09 |
| 卷号 | 30期号:9页码:1344-1350 |
| 关键词 | 11 beta-hydroxysteroid dehydrogenase type 1 inhibitors molecular modeling |
| ISSN号 | 1671-4083 |
| DOI | 10.1038/aps.2009.118 |
| 文献子类 | Article |
| 英文摘要 | Aim: To design and synthese a novel class of 11 beta-hydroxysteroid dehydrogenase type 1 (11 beta-HSD1) inhibitors, featuring the (phenylsulfonamido-methyl)pyridine and (phenylsulfonamido-methyl)thiazole framework. Methods: Our initial lead 4-(phenylsulfonamido-methyl)benzamides were modified. Inhibition of human and mouse 11 beta-HSD1 enzymatic activities by the new compounds was determined by a scintillation proximity assay (SPA) using microsomes containing 11 beta-HSD1. Results: Sixteen new compounds (6a-6h, 7a-7h) were designed, synthesized and bioassayed. In dose-response studies, several compounds showed strong inhibitory activities with IC50 values at nanomolar or low nanomolar concentrations. Structure-activity relationships are also discussed with respect to molecular docking results. Conclusion: This study provides two promising new templates for 11 beta-HSD1 inhibitors. |
| WOS关键词 | METABOLIC SYNDROME ; VISCERAL OBESITY ; MICE ; IDENTIFICATION |
| 资助项目 | National Basic Research Program of China[2009CB522300] ; National Natural Science Foundation of China[90813029] ; Science and Technology Commission of Shanghai Municipality[08QH14028] ; Science and Technology Commission of Shanghai Municipality[08ZR1422600] |
| WOS研究方向 | Chemistry ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| CSCD记录号 | CSCD:3672210 |
| WOS记录号 | WOS:000269894400017 |
| 出版者 | ACTA PHARMACOLOGICA SINICA |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/279139]  |
| 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, Yang,Shen, Yu,et al. Derivatives of (phenylsulfonamido-methyl)nicotine and (phenylsulfonamido-methyl)thiazole as novel 11 beta-hydroxysteroid dehydrogenase type 1 inhibitors: synthesis and biological activities in vitro[J]. ACTA PHARMACOLOGICA SINICA,2009,30(9):1344-1350. |
| APA | Zhang, Xu.,Zhou, Yang.,Shen, Yu.,Du, Li-li.,Chen, Jun-hua.,...&Shen, Jian-hua.(2009).Derivatives of (phenylsulfonamido-methyl)nicotine and (phenylsulfonamido-methyl)thiazole as novel 11 beta-hydroxysteroid dehydrogenase type 1 inhibitors: synthesis and biological activities in vitro.ACTA PHARMACOLOGICA SINICA,30(9),1344-1350. |
| MLA | Zhang, Xu,et al."Derivatives of (phenylsulfonamido-methyl)nicotine and (phenylsulfonamido-methyl)thiazole as novel 11 beta-hydroxysteroid dehydrogenase type 1 inhibitors: synthesis and biological activities in vitro".ACTA PHARMACOLOGICA SINICA 30.9(2009):1344-1350. |
入库方式： OAI收割
来源：上海药物研究所
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