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Bioorg Med Chem Lett ; 19(1): 158-62, 2009 Jan 01.
Article in English | MEDLINE | ID: mdl-19019676

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).


Subject(s)
Benzamides/chemical synthesis , Pyrazoles/chemical synthesis , Receptors, Glucocorticoid/agonists , Administration, Oral , Animals , Benzamides/pharmacology , Humans , Hydrophobic and Hydrophilic Interactions , Prednisolone , Pyrazoles/pharmacology , Rats , Structure-Activity Relationship
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