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).
MeSH terms
-
Administration, Oral
-
Animals
-
Benzamides / chemical synthesis*
-
Benzamides / pharmacology
-
Humans
-
Hydrophobic and Hydrophilic Interactions
-
Prednisolone
-
Pyrazoles / chemical synthesis*
-
Pyrazoles / pharmacology
-
Rats
-
Receptors, Glucocorticoid / agonists*
-
Structure-Activity Relationship
Substances
-
Benzamides
-
Pyrazoles
-
Receptors, Glucocorticoid
-
Prednisolone