title: 5-Functionalized indazoles as glucocorticoid receptor agonists.
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.
authors.affiliation: AMRI, Albany, NY 12212-5098, USA.
authors.forename: Mei
authors.initials: M
authors.lastname: Bai
authors.forename: Grant
authors.initials: G
authors.lastname: Carr
authors.forename: Russell J
authors.initials: RJ
authors.lastname: Deorazio
authors.forename: Thomas D
authors.initials: TD
authors.lastname: Friedrich
authors.forename: Svetlana
authors.initials: S
authors.lastname: Dobritsa
authors.forename: Kevin
authors.initials: K
authors.lastname: Fitzpatrick
authors.forename: Peter R
authors.initials: PR
authors.lastname: Guzzo
authors.forename: Douglas B
authors.initials: DB
authors.lastname: Kitchen
authors.forename: Michael A
authors.initials: MA
authors.lastname: Lynch
authors.forename: Denise
authors.initials: D
authors.lastname: Peace
authors.forename: Mohammed
authors.initials: M
authors.lastname: Sajad
authors.forename: Alexander
authors.initials: A
authors.lastname: Usyatinsky
authors.forename: Mark A
authors.initials: MA
authors.lastname: Wolf
mesh_terms: D000818:Animals; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D007191:Indazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D051379:Mice; D011965:Receptors, Glucocorticoid / Q000819:agonists* / Q000378:metabolism; D014409:Tumor Necrosis Factor-alpha / Q000378:metabolism
chemical_list: D000893:Anti-Inflammatory Agents; D007191:Indazoles; D011965:Receptors, Glucocorticoid; D014409:Tumor Necrosis Factor-alpha