| Literature DB >> 20427184 |
Mei Bai1, Grant Carr, Russell J Deorazio, Thomas D Friedrich, Svetlana Dobritsa, Kevin Fitzpatrick, Peter R Guzzo, Douglas B Kitchen, Michael A Lynch, Denise Peace, Mohammed Sajad, Alexander Usyatinsky, Mark A Wolf.
Abstract
An indazole based series of glucocorticoid receptor agonists is reported. The SAR exploration of this scaffold yielded compounds with nanomolar affinity for the glucocorticoid receptor with indications of selectivity for the preferred transrepression mechanism; in vivo efficacy was observed in the mouse LPS induced TNFalpha model for compound 28. Copyright 2010 Elsevier Ltd. All rights reserved.Entities:
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Year: 2010 PMID： 20427184 DOI： 10.1016/j.bmcl.2010.04.012
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823