title: 2-Arylbenzoxazoles as CETP inhibitors: raising HDL-C in cynoCETP transgenic mice.
abstract: We describe structure-activity studies leading to the discovery of 2-arylbenzoxazole 3, the first in a series to raise serum high-density lipoprotein cholesterol levels in transgenic mice. Replacement of the 4-piperidinyloxy moiety with piperazinyl provided a more synthetically tractable lead, which upon optimization resulted in compound 4, an excellent inhibitor of cholesteryl ester transfer protein function with good pharmacokinetic properties and in vivo efficacy.
authors.affiliation: Merck Research Laboratories, Rahway, NJ 07065, USA. florida_kallashi@merck.com
authors.forename: Florida
authors.initials: F
authors.lastname: Kallashi
authors.forename: Dooseop
authors.initials: D
authors.lastname: Kim
authors.forename: Jennifer
authors.initials: J
authors.lastname: Kowalchick
authors.forename: You Jung
authors.initials: YJ
authors.lastname: Park
authors.forename: Julianne A
authors.initials: JA
authors.lastname: Hunt
authors.forename: Amjad
authors.initials: A
authors.lastname: Ali
authors.forename: Cameron J
authors.initials: CJ
authors.lastname: Smith
authors.forename: Milton L
authors.initials: ML
authors.lastname: Hammond
authors.forename: James V
authors.initials: JV
authors.lastname: Pivnichny
authors.forename: Xinchun
authors.initials: X
authors.lastname: Tong
authors.forename: Suoyu S
authors.initials: SS
authors.lastname: Xu
authors.forename: Matt S
authors.initials: MS
authors.lastname: Anderson
authors.forename: Ying
authors.initials: Y
authors.lastname: Chen
authors.forename: Suzanne S
authors.initials: SS
authors.lastname: Eveland
authors.forename: Qiu
authors.initials: Q
authors.lastname: Guo
authors.forename: Sheryl A
authors.initials: SA
authors.lastname: Hyland
authors.forename: Denise P
authors.initials: DP
authors.lastname: Milot
authors.forename: Anne-Marie
authors.initials: AM
authors.lastname: Cumiskey
authors.forename: Melanie
authors.initials: M
authors.lastname: Latham
authors.forename: Laurence B
authors.initials: LB
authors.lastname: Peterson
authors.forename: Raymond
authors.initials: R
authors.lastname: Rosa
authors.forename: Carl P
authors.initials: CP
authors.lastname: Sparrow
authors.forename: Samuel D
authors.initials: SD
authors.lastname: Wright
authors.forename: Peter J
authors.initials: PJ
authors.lastname: Sinclair
mesh_terms: D000083:Acetanilides / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D000818:Animals; D001583:Benzoxazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D053480:Cholesterol Ester Transfer Proteins / Q000037:antagonists & inhibitors* / Q000378:metabolism; D008076:Cholesterol, HDL / Q000097:blood*; D051379:Mice; D008822:Mice, Transgenic; D013329:Structure-Activity Relationship
chemical_list: D000083:Acetanilides; D001583:Benzoxazoles; D053480:Cholesterol Ester Transfer Proteins; D008076:Cholesterol, HDL