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

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

来源：Bioorganic & Medicinal Chemistry Letters, 2009, 19(1): 158-162.

DOI：10.1016/j.bmcl.2008.10.128

• GR
• Glucocorticoid
• Aminopyrazole

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).

• 出版日期2009-1-1