title: 3-(3-Aryloxyaryl)imidazo[1,2-a]pyridine sulfones as liver X receptor agonists.
abstract: Replacement of a quinoline with an imidazo[1,2-a]pyridine in a series of liver X receptor (LXR) agonists incorporating a [3-(sulfonyl)aryloxyphenyl] side chain provided high affinity LXR ligands 7. In functional assays of LXR activity, good agonist potency and efficacy were found for several analogs.
authors.affiliation: Chemical Sciences, Wyeth Pharmaceuticals, 500 Arcola Rd., Collegeville, PA 19426, USA. Singhar@wyeth.com
authors.forename: Robert R
authors.initials: RR
authors.lastname: Singhaus
authors.forename: Ronald C
authors.initials: RC
authors.lastname: Bernotas
authors.forename: Robert
authors.initials: R
authors.lastname: Steffan
authors.forename: Edward
authors.initials: E
authors.lastname: Matelan
authors.forename: Elaine
authors.initials: E
authors.lastname: Quinet
authors.forename: Ponnal
authors.initials: P
authors.lastname: Nambi
authors.forename: Irene
authors.initials: I
authors.lastname: Feingold
authors.forename: Christine
authors.initials: C
authors.lastname: Huselton
authors.forename: Anna
authors.initials: A
authors.lastname: Wilhelmsson
authors.forename: Annika
authors.initials: A
authors.lastname: Goos-Nilsson
authors.forename: Jay
authors.initials: J
authors.lastname: Wrobel
mesh_terms: D018528:ATP-Binding Cassette Transporters / Q000235:genetics / Q000378:metabolism; D000818:Animals; D056945:Hep G2 Cells; D006801:Humans; D000071518:Liver X Receptors; D051379:Mice; D008862:Microsomes, Liver / Q000378:metabolism; D057093:Orphan Nuclear Receptors / Q000819:agonists* / Q000378:metabolism; D011485:Protein Binding; D011725:Pyridines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011804:Quinolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D012333:RNA, Messenger / Q000378:metabolism; D013329:Structure-Activity Relationship; D013450:Sulfones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
chemical_list: D018528:ATP-Binding Cassette Transporters; D000071518:Liver X Receptors; D057093:Orphan Nuclear Receptors; D011725:Pyridines; D011804:Quinolines; D012333:RNA, Messenger; D013450:Sulfones; C023666:pyridine