中国科学院机构知识库网格
Chinese Academy of Sciences Institutional Repositories Grid
derivativesofphenylsulfonamidomethylnicotineandphenylsulfonamidomethylthiazoleasnovel11hydroxysteroiddehydrogenasetype1inhibitorssynthesisandbiologicalactivitiesinvitro

文献类型:期刊论文

作者Xu ZHANG; Yang ZHOU; Yu SHEN; Lili DU; Junhua CHEN; Ying LENG; Jianhua SHEN
刊名actapharmacologicasinica
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/2S10ELR8/287189]  
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
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Xu ZHANG,Yang ZHOU,Yu SHEN,et al. derivativesofphenylsulfonamidomethylnicotineandphenylsulfonamidomethylthiazoleasnovel11hydroxysteroiddehydrogenasetype1inhibitorssynthesisandbiologicalactivitiesinvitro[J]. actapharmacologicasinica,2009,000(009):1344.
APA Xu ZHANG.,Yang ZHOU.,Yu SHEN.,Lili DU.,Junhua CHEN.,...&Jianhua SHEN.(2009).derivativesofphenylsulfonamidomethylnicotineandphenylsulfonamidomethylthiazoleasnovel11hydroxysteroiddehydrogenasetype1inhibitorssynthesisandbiologicalactivitiesinvitro.actapharmacologicasinica,000(009),1344.
MLA Xu ZHANG,et al."derivativesofphenylsulfonamidomethylnicotineandphenylsulfonamidomethylthiazoleasnovel11hydroxysteroiddehydrogenasetype1inhibitorssynthesisandbiologicalactivitiesinvitro".actapharmacologicasinica 000.009(2009):1344.

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来源:上海药物研究所

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