5-Functionalized indazoles as glucocorticoid receptor agonists

Autor:	Douglas B. Kitchen, Svetlana Dobritsa, Mei Bai, Thomas D. Friedrich, Peter R. Guzzo, Grant J. Carr, Mark A. Wolf, Michael A. Lynch, Alexander Usyatinsky, Russell J. DeOrazio, Denise Peace, Kevin Fitzpatrick, Mohammed Sajad
Rok vydání:	2010
Předmět:	Agonist Indazoles medicine.drug_class Clinical Biochemistry Anti-Inflammatory Agents Pharmaceutical Science Pharmacology Biochemistry Chemical synthesis Mice Transactivation chemistry.chemical_compound Receptors Glucocorticoid Glucocorticoid receptor In vivo Drug Discovery medicine Animals Molecular Biology Transrepression Indazole Tumor Necrosis Factor-alpha Organic Chemistry In vitro chemistry Molecular Medicine
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 20:3017-3020
ISSN:	0960-894X
DOI:	10.1016/j.bmcl.2010.04.012
Popis:	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 TNFα model for compound 28.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cf658724c2cf779a78fc64c6106b32be https://doi.org/10.1016/j.bmcl.2010.04.012 Zobrazit plný text záznamu Full Text from ScienceDirect