Literature DB >> 19019676

Aryl aminopyrazole benzamides as oral non-steroidal selective glucocorticoid receptor agonists.

Heather A Barnett1, Diane M Coe, Tony W J Cooper, Torquil I Jack, Haydn T Jones, Simon J F Macdonald, Iain M McLay, Natalie Rayner, Rosemary Z Sasse, Tracy J Shipley, Phil A Skone, Graham I Somers, Simon Taylor, Iain J Uings, James M Woolven, Gordon G Weingarten.   

Abstract

Aryl aminopyrazole amides capped with N-alkylbenzamides 13-16 are selective glucocorticoid receptor agonists. 2,6-Disubstituted benzamides have prednisolone-like potency or better in vitro. Good oral exposure was demonstrated in the rat, with compounds with lower lipophilicity, for example N-hydroxyethyl benzamides (e.g., 16e).

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Year:  2008        PMID: 19019676     DOI: 10.1016/j.bmcl.2008.10.128

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


  1 in total

1.  Design and x-ray crystal structures of high-potency nonsteroidal glucocorticoid agonists exploiting a novel binding site on the receptor.

Authors:  Keith Biggadike; Randy K Bledsoe; Diane M Coe; Tony W J Cooper; David House; Marie A Iannone; Simon J F Macdonald; Kevin P Madauss; Iain M McLay; Tracy J Shipley; Simon J Taylor; Thuy B Tran; Iain J Uings; Victoria Weller; Shawn P Williams
Journal:  Proc Natl Acad Sci U S A       Date:  2009-10-12       Impact factor: 11.205

  1 in total

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