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
Respiratory CEDD, Medicines Research Centre, Stevenage, UK.
Bioorg Med Chem Lett. 2009 Jan 1;19(1):158-62. doi: 10.1016/j.bmcl.2008.10.128. Epub 2008 Nov 5.
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).
带有N-烷基苯甲酰胺的芳基氨基吡唑酰胺13-16是选择性糖皮质激素受体激动剂。2,6-二取代苯甲酰胺在体外具有类似泼尼松龙的效力或更好的效力。在大鼠中证明了良好的口服暴露，对于亲脂性较低的化合物，例如N-羟乙基苯甲酰胺（例如16e）。
