title: Heterocyclic glucocorticoid receptor modulators with a 2,2-dimethyl-3-phenyl-N-(thiazol or thiadiazol-2-yl)propanamide core.
abstract: A series of heterocyclic glucocorticoid receptor (GR) modulators with 2,2-dimethyl-3-phenyl-N-(thiazol or thiadiazol-2-yl)propanamide core are described. Structure-activity relationships suggest a combination of H-bond acceptor and a 4-fluorophenyl moiety as being important structural components contributing to the glucocorticoid receptor binding and functional activity for this series of GR modulators.
authors.affiliation: Research and Development, Bristol-Myers Squibb Company, Princeton, NJ 08543-4000, United States.
authors.forename: Hai-Yun
authors.initials: HY
authors.lastname: Xiao
authors.forename: Dauh-Rurng
authors.initials: DR
authors.lastname: Wu
authors.forename: James E
authors.initials: JE
authors.lastname: Sheppeck
authors.forename: Sium F
authors.initials: SF
authors.lastname: Habte
authors.forename: Mark D
authors.initials: MD
authors.lastname: Cunningham
authors.forename: John E
authors.initials: JE
authors.lastname: Somerville
authors.forename: Joel C
authors.initials: JC
authors.lastname: Barrish
authors.forename: Steven G
authors.initials: SG
authors.lastname: Nadler
authors.forename: T G Murali
authors.initials: TG
authors.lastname: Dhar
mesh_terms: D000577:Amides / Q000737:chemistry*; D006571:Heterocyclic Compounds / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism; D011485:Protein Binding; D011965:Receptors, Glucocorticoid / Q000819:agonists* / Q000378:metabolism; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D013830:Thiadiazoles / Q000737:chemistry*; D013844:Thiazoles / Q000737:chemistry*
chemical_list: D000577:Amides; D006571:Heterocyclic Compounds; D011965:Receptors, Glucocorticoid; D013830:Thiadiazoles; D013844:Thiazoles
keywords: Dissociated steroids; Glucocorticoid receptor; Non-steroidal glucocorticoid receptor agonists; Transactivation; Transrepression