Literature DB >> 21439819

Pyrrolidine-pyrazole ureas as potent and selective inhibitors of 11β-hydroxysteroid-dehydrogenase type 1.

Olivier Venier1, Cécile Pascal, Alain Braun, Claudie Namane, Patrick Mougenot, Olivier Crespin, François Pacquet, Cécile Mougenot, Catherine Monseau, Bénédicte Onofri, Rommel Dadji-Faïhun, Céline Leger, Majdi Ben-Hassine, Thao Van-Pham, Jean-Luc Ragot, Christophe Philippo, Stefan Güssregen, Christian Engel, Géraldine Farjot, Lionel Noah, Karima Maniani, Eric Nicolaï.   

Abstract

A High Throughput Screening campaign allowed the identification of a novel class of ureas as 11β-HSD1 inhibitors. Rational chemical optimization provided potent and selective inhibitors of both human and murine 11β-HSD1 with an appropriate ADME profile and ex vivo activity in target tissues.
Copyright © 2011 Elsevier Ltd. All rights reserved.

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Year:  2011        PMID: 21439819     DOI: 10.1016/j.bmcl.2011.02.111

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


  2 in total

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Authors:  Zhao-Kui Wan; Eva Chenail; Huan-Qiu Li; Manus Ipek; Jason Xiang; Vipin Suri; Seung Hahm; Joel Bard; Kristine Svenson; Xin Xu; Xianbin Tian; Mengmeng Wang; Xiangping Li; Christian E Johnson; Ariful Qadri; Darrell Panza; Mylene Perreault; Tarek S Mansour; James F Tobin; Eddine Saiah
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Authors:  Michelle D Cherne; Jesse Hall; Alisha Kellner; Christine F Chong; Amy L Cole; Alexander M Cole
Journal:  Viruses       Date:  2019-05-01       Impact factor: 5.048

  2 in total

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