title: 2-Arylbenzoxazoles as CETP inhibitors: Substitution of the benzoxazole moiety.
abstract: A series of 2-arylbenzoxazole inhibitors of the cholesterol ester transfer protein (CETP) is described. Structure-activity studies focused on variation of the substitution of the benzoxazole moiety. Substitution at the 5- and 7-positions of the benzoxazole moiety was found to be beneficial for CETP inhibition. Compound 47 was found to be the most potent inhibitor in this series and inhibited CETP with an IC(50) of 28nM.
authors.affiliation: Department of Medicinal Chemistry, Merck Research Laboratories, Rahway NJ 07065, United States. cameron_smith@merck.com
authors.forename: Cameron J
authors.initials: CJ
authors.lastname: Smith
authors.forename: Amjad
authors.initials: A
authors.lastname: Ali
authors.forename: Liya
authors.initials: L
authors.lastname: Chen
authors.forename: Milton L
authors.initials: ML
authors.lastname: Hammond
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: D000083:Acetanilides / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D000284:Administration, Oral; D000818:Animals; D000924:Anticholesteremic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D001583:Benzoxazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D053480:Cholesterol Ester Transfer Proteins / Q000037:antagonists & inhibitors* / Q000378:metabolism; D051379:Mice; D013329:Structure-Activity Relationship
chemical_list: D000083:Acetanilides; D000924:Anticholesteremic Agents; D001583:Benzoxazoles; D053480:Cholesterol Ester Transfer Proteins