title: Novel heterocyclic glucocorticoids: in vitro profile and in vivo efficacy.
abstract: A series of novel ligands for the glucocorticoid receptor containing two heterocycles were synthesized. These compounds were investigated for a dissociative profile using transrepression and transactivation assays. Several compounds were tested in vivo and showed the ability to reduce inflammation in a mouse.
authors.affiliation: Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA. christopher_thompson@merck.com <christopher_thompson@merck.com>
authors.forename: Christopher F
authors.initials: CF
authors.lastname: Thompson
authors.forename: Nazia
authors.initials: N
authors.lastname: Quraishi
authors.forename: Amjad
authors.initials: A
authors.lastname: Ali
authors.forename: James R
authors.initials: JR
authors.lastname: Tata
authors.forename: Milton L
authors.initials: ML
authors.lastname: Hammond
authors.forename: James M
authors.initials: JM
authors.lastname: Balkovec
authors.forename: Monica
authors.initials: M
authors.lastname: Einstein
authors.forename: Lan
authors.initials: L
authors.lastname: Ge
authors.forename: Georgianna
authors.initials: G
authors.lastname: Harris
authors.forename: Theresa M
authors.initials: TM
authors.lastname: Kelly
authors.forename: Paul
authors.initials: P
authors.lastname: Mazur
authors.forename: Shilpa
authors.initials: S
authors.lastname: Pandit
authors.forename: Joseph
authors.initials: J
authors.lastname: Santoro
authors.forename: Ayesha
authors.initials: A
authors.lastname: Sitlani
authors.forename: Chuanlin
authors.initials: C
authors.lastname: Wang
authors.forename: Joanne
authors.initials: J
authors.lastname: Williamson
authors.forename: Douglas K
authors.initials: DK
authors.lastname: Miller
authors.forename: Ting-ting D
authors.initials: TT
authors.lastname: Yamin
authors.forename: Chris M
authors.initials: CM
authors.lastname: Thompson
authors.forename: Edward A
authors.initials: EA
authors.lastname: O'Neill
authors.forename: Dennis
authors.initials: D
authors.lastname: Zaller
authors.forename: Michael J
authors.initials: MJ
authors.lastname: Forrest
authors.forename: Ester
authors.initials: E
authors.lastname: Carballo-Jane
authors.forename: Silvi
authors.initials: S
authors.lastname: Luell
mesh_terms: D000818:Animals; D000893:Anti-Inflammatory Agents / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology; D002460:Cell Line; D005938:Glucocorticoids / Q000008:administration & dosage / Q000737:chemistry* / Q000494:pharmacology; D006571:Heterocyclic Compounds / Q000008:administration & dosage / Q000737:chemistry* / Q000494:pharmacology; D006801:Humans; D008070:Lipopolysaccharides / Q000494:pharmacology; D051379:Mice; D008810:Mice, Inbred C57BL; D051381:Rats; D014409:Tumor Necrosis Factor-alpha / Q000037:antagonists & inhibitors / Q000096:biosynthesis
chemical_list: D000893:Anti-Inflammatory Agents; D005938:Glucocorticoids; D006571:Heterocyclic Compounds; D008070:Lipopolysaccharides; D014409:Tumor Necrosis Factor-alpha