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

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Barnett HA, Coe DM, Cooper TW, Jack TI, Jones HT, Macdonald SJ, McLay IM, Rayner N, Sasse RZ, Shipley TJ, Skone PA, Somers GI, Taylor S, Uings IJ, Woolven JM, Weingarten GG

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

Bioorg Med Chem Lett. 2009 Jan 1;19(1):158-62. doi: 10.1016/j.bmcl.2008.10.128. Epub 2008 Nov 5.

PubMed ID

19019676 [ View in PubMed

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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).

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Prednisolone	Glucocorticoid receptor	EC 50 (nM)	50.12	N/A	N/A	Details
Prednisolone	Glucocorticoid receptor	IC 50 (nM)	12.59	N/A	N/A	Details