| Literature DB >> 21073190 |
Bingwei V Yang1, David S Weinstein, Lidia M Doweyko, Hua Gong, Wayne Vaccaro, Tram Huynh, Hai-Yun Xiao, Arthur M Doweyko, Lorraine McKay, Deborah A Holloway, John E Somerville, Sium Habte, Mark Cunningham, Michele McMahon, Robert Townsend, David Shuster, John H Dodd, Steven G Nadler, Joel C Barrish.
Abstract
A series of 2,2-dimethyl-3,3-diphenyl-propanamides as novel glucocorticoid receptor modulators is reported. SAR exploration led to the identification of 4-hydroxyphenyl propanamide derivatives displaying good agonist activity in GR-mediated transrepression assays and reduced agonist activity in GR-mediated transactivation assays. Compounds 17 and 30 showed anti-inflammatory activity comparable to prednisolone in the rat carrageenan-induced paw edema model, with markedly decreased side effects with regard to increases in blood glucose and expression of hepatic tyrosine aminotransferase. A hypothetical binding mode accounting for the induction of the functional activity by a 4-hydroxyl group is proposed.Entities:
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Year: 2010 PMID： 21073190 DOI： 10.1021/jm100957a
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446