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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 benzamides as oral non-steroidal selective glucocorticoid receptor agonists.

Author information

1
Respiratory CEDD, Medicines Research Centre, Stevenage, UK.

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).

PMID:
19019676
DOI:
10.1016/j.bmcl.2008.10.128
[Indexed for MEDLINE]

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