title: Aryl aminopyrazole benzamides as oral non-steroidal selective glucocorticoid receptor agonists.
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).
authors.affiliation: Respiratory CEDD, Medicines Research Centre, Stevenage, UK.
authors.forename: Heather A
authors.initials: HA
authors.lastname: Barnett
authors.forename: Diane M
authors.initials: DM
authors.lastname: Coe
authors.forename: Tony W J
authors.initials: TW
authors.lastname: Cooper
authors.forename: Torquil I
authors.initials: TI
authors.lastname: Jack
authors.forename: Haydn T
authors.initials: HT
authors.lastname: Jones
authors.forename: Simon J F
authors.initials: SJ
authors.lastname: Macdonald
authors.forename: Iain M
authors.initials: IM
authors.lastname: McLay
authors.forename: Natalie
authors.initials: N
authors.lastname: Rayner
authors.forename: Rosemary Z
authors.initials: RZ
authors.lastname: Sasse
authors.forename: Tracy J
authors.initials: TJ
authors.lastname: Shipley
authors.forename: Phil A
authors.initials: PA
authors.lastname: Skone
authors.forename: Graham I
authors.initials: GI
authors.lastname: Somers
authors.forename: Simon
authors.initials: S
authors.lastname: Taylor
authors.forename: Iain J
authors.initials: IJ
authors.lastname: Uings
authors.forename: James M
authors.initials: JM
authors.lastname: Woolven
authors.forename: Gordon G
authors.initials: GG
authors.lastname: Weingarten
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001549:Benzamides / Q000138:chemical synthesis* / Q000494:pharmacology; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D011239:Prednisolone; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats; D011965:Receptors, Glucocorticoid / Q000819:agonists*; D013329:Structure-Activity Relationship
chemical_list: D001549:Benzamides; D011720:Pyrazoles; D011965:Receptors, Glucocorticoid; D011239:Prednisolone