Derivatives of （phenylsulfonamido-methyl）nicotine and （phenylsulfonamido-methyl）thiazole as novel 11β-hydroxysteroid dehydrogenase type 1 inhibitors： synthesis and biological activities in vitro
文献类型：期刊论文
| 作者 | Xu ZHANG; Yang ZHOU; Yu SHEN; Lili DU; Junhua CHEN; Ying LENG ; Jianhua SHEN
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| 刊名 | 中国药理学报：英文版
 |
| 出版日期 | 2009 |
| 卷号 | 000期号:009页码:1344 |
| 关键词 | 醇脱氢酶 抑制剂 合成酶 生物活性 噻唑 1型 基类 衍生物 |
| ISSN号 | 1671-4083 |
| 英文摘要 | Aim： To design and synthese a novel class of 11β-hydroxysteroid dehydrogenase type 1 （11β-HSD1） inhibitors, featuring the （phenylsul- fonamido-methyl）pyridine and （phenylsulfonamido-methyl）thiazole framework. Methods： Our initial lead 4-（phenylsulfonamido-methyl）benzamides were modified. Inhibition of human and mouse 11β-HSD1 enzymatic activities by the new compounds was determined by a scintillation proximity assay （SPA） using microsomes containing 11β- HSDI. 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 11β-HSD1 inhibitors. |
| 语种 | 英语 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/295060]  |
| 专题 | 中国科学院上海药物研究所 |
| 作者单位 | 中国科学院上海药物研究所 |
| 推荐引用方式 GB/T 7714 | Xu ZHANG,Yang ZHOU,Yu SHEN,等. Derivatives of （phenylsulfonamido-methyl）nicotine and （phenylsulfonamido-methyl）thiazole as novel 11β-hydroxysteroid dehydrogenase type 1 inhibitors： synthesis and biological activities in vitro[J]. 中国药理学报：英文版,2009,000(009):1344. |
| APA | Xu ZHANG.,Yang ZHOU.,Yu SHEN.,Lili DU.,Junhua CHEN.,...&Jianhua SHEN.(2009).Derivatives of （phenylsulfonamido-methyl）nicotine and （phenylsulfonamido-methyl）thiazole as novel 11β-hydroxysteroid dehydrogenase type 1 inhibitors： synthesis and biological activities in vitro.中国药理学报：英文版,000(009),1344. |
| MLA | Xu ZHANG,et al."Derivatives of （phenylsulfonamido-methyl）nicotine and （phenylsulfonamido-methyl）thiazole as novel 11β-hydroxysteroid dehydrogenase type 1 inhibitors： synthesis and biological activities in vitro".中国药理学报：英文版 000.009(2009):1344. |
入库方式： OAI收割
来源：上海药物研究所
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