title: SAR studies: designing potent and selective LXR agonists.
abstract: Counterscreening compounds from a Merck PPAR program discovered lead 1, as a nanomolar LXR/PPAR dual agonist. SAR optimization developed a series of heterocyclic LXR agonists having excellent selectivity over all PPAR isoforms and possessing high LXR affinity and strong in vivo potency.
authors.affiliation: Department of Medicinal Chemistry, Merck Research Laboratories, Merck & Co., Inc., PO Box 2000, Rahway, NJ 07065, USA. jason_szewczyk@merck.com
authors.forename: Jason W
authors.initials: JW
authors.lastname: Szewczyk
authors.forename: Shaei
authors.initials: S
authors.lastname: Huang
authors.forename: Jayne
authors.initials: J
authors.lastname: Chin
authors.forename: Jenny
authors.initials: J
authors.lastname: Tian
authors.forename: Lyndon
authors.initials: L
authors.lastname: Mitnaul
authors.forename: Raymond L
authors.initials: RL
authors.lastname: Rosa
authors.forename: Larry
authors.initials: L
authors.lastname: Peterson
authors.forename: Carl P
authors.initials: CP
authors.lastname: Sparrow
authors.forename: Alan D
authors.initials: AD
authors.lastname: Adams
mesh_terms: D000143:Acids / Q000737:chemistry; D000586:Amination; D000814:Aniline Compounds / Q000737:chemistry; D000818:Animals; D008076:Cholesterol, HDL / Q000097:blood; D003500:Cyclization; D004268:DNA-Binding Proteins / Q000819:agonists*; D015195:Drug Design; D007211:Indoles / Q000737:chemistry; D000071518:Liver X Receptors; D051379:Mice; D015394:Molecular Structure; D057093:Orphan Nuclear Receptors; D018160:Receptors, Cytoplasmic and Nuclear / Q000819:agonists*; D013329:Structure-Activity Relationship
chemical_list: D000143:Acids; D000814:Aniline Compounds; D008076:Cholesterol, HDL; D004268:DNA-Binding Proteins; D007211:Indoles; D000071518:Liver X Receptors; D057093:Orphan Nuclear Receptors; D018160:Receptors, Cytoplasmic and Nuclear; C023650:aniline