3-(3-Aryloxyaryl)imidazo[1,2-a]pyridine sulfones as liver X receptor agonists.
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.
Singhaus
Robert R
RR
Chemical Sciences, Wyeth Pharmaceuticals, 500 Arcola Rd., Collegeville, PA 19426, USA. Singhar@wyeth.com
Bernotas
Ronald C
RC
Steffan
Robert
R
Matelan
Edward
E
Quinet
Elaine
E
Nambi
Ponnal
P
Feingold
Irene
I
Huselton
Christine
C
Wilhelmsson
Anna
A
Goos-Nilsson
Annika
A
Wrobel
Jay
J
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
D018528:ATP-Binding Cassette Transporters; D000071518:Liver X Receptors; D057093:Orphan Nuclear Receptors; D011725:Pyridines; D011804:Quinolines; D012333:RNA, Messenger; D013450:Sulfones; C023666:pyridine