Literature DB >> 18511278

Discovery and initial SAR of arylsulfonylpiperazine inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1).

Daqing Sun1, Zhulun Wang, Yongmei Di, Juan C Jaen, Marc Labelle, Ji Ma, Shichang Miao, Athena Sudom, Liang Tang, Craig S Tomooka, Hua Tu, Stefania Ursu, Nigel Walker, Xuelei Yan, Qiuping Ye, Jay P Powers.   

Abstract

High-throughput screening of a small-molecule compound library resulted in the identification of a series of arylsulfonylpiperazines that are potent and selective inhibitors of human 11beta-Hydroxysteroid Dehydrogenase Type 1 (11beta-HSD1). Optimization of the initial lead resulted in the discovery of compound (R)-45 (11beta-HSD1 IC(50)=3nM).

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Year:  2008        PMID: 18511278     DOI: 10.1016/j.bmcl.2008.05.025

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  4 in total

1.  On-column ligand exchange for structure-based drug design: a case study with human 11β-hydroxysteroid dehydrogenase type 1.

Authors:  Wenying Qin; Russell A Judge; Kenton L Longenecker; Larry R Solomon; John E Harlan
Journal:  Acta Crystallogr Sect F Struct Biol Cryst Commun       Date:  2012-04-21

2.  Correctors and Potentiators Rescue Function of the Truncated W1282X-Cystic Fibrosis Transmembrane Regulator (CFTR) Translation Product.

Authors:  Peter M Haggie; Puay-Wah Phuan; Joseph-Anthony Tan; Haijin Xu; Radu G Avramescu; Doranda Perdomo; Lorna Zlock; Dennis W Nielson; Walter E Finkbeiner; Gergely L Lukacs; Alan S Verkman
Journal:  J Biol Chem       Date:  2016-11-28       Impact factor: 5.157

Review 3.  Crystal structures of 11β-hydroxysteroid dehydrogenase type 1 and their use in drug discovery.

Authors:  Mark P Thomas; Barry V L Potter
Journal:  Future Med Chem       Date:  2011-03       Impact factor: 3.808

4.  Identification of important chemical features of 11β-hydroxysteroid dehydrogenase type1 inhibitors: application of ligand based virtual screening and density functional theory.

Authors:  Sugunadevi Sakkiah; Chandrasekaran Meganathan; Young-Sik Sohn; Sundaraganesan Namadevan; Keun Woo Lee
Journal:  Int J Mol Sci       Date:  2012-04-23       Impact factor: 6.208

  4 in total

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