title: 2-Arylbenzoxazoles as CETP inhibitors: substitution and modification of the alpha-alkoxyamide moiety.
abstract: The development of a series of 2-arylbenzoxazole alpha-alkoxyamide and beta-alkoxyamine inhibitors of cholesteryl ester transfer protein (CETP) is described. Highly fluorinated alpha-alkoxyamides proved to be potent inhibitors of CETP in vitro, and the highly fluorinated 2-arylbenzoxazole beta-alkoxyamine 4 showed a desirable combination of in vitro potency (IC(50)=151 nM) and oral bioavailability in the mouse.
authors.affiliation: Merck Research Laboratories, Rahway, NJ 07065, United States.
authors.forename: Julianne A
authors.initials: JA
authors.lastname: Hunt
authors.forename: Silvia
authors.initials: S
authors.lastname: Gonzalez
authors.forename: Florida
authors.initials: F
authors.lastname: Kallashi
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: 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: D000438:Alcohols / Q000138:chemical synthesis / Q000378:metabolism; D000577:Amides / Q000138:chemical synthesis / Q000378:metabolism; D001583:Benzoxazoles / Q000138:chemical synthesis* / Q000378:metabolism*; D053480:Cholesterol Ester Transfer Proteins / Q000037:antagonists & inhibitors* / Q000378:metabolism*
chemical_list: D000438:Alcohols; D000577:Amides; D001583:Benzoxazoles; C506642:CETP protein, human; D053480:Cholesterol Ester Transfer Proteins; C059688:alkoxyl radical