title: Discovery of substituted biphenyl oxazolidinone inhibitors of cholesteryl ester transfer protein.
abstract: Recently, there has been a strong interest in the ability to increase levels of high density lipoprotein-cholesterol (HDL-C). This interest stems from the hypothesis that such an elevation in HDL-C will decrease the likelihood of cardiovascular disease. Inhibition of cholesteryl ester transfer protein (CETP) has been shown to elevate HDL-C levels in human subjects. This letter describes the discovery of a novel and potent (<100 nM IC50 for the inhibition of CE transfer) CETP inhibitor scaffold containing an oxazolidinone core.
authors.affiliation: Departments of Medicinal Chemistry and Cardiovascular Diseases, Merck Research Laboratories , Rahway, New Jersey 07065, United States.
authors.forename: Christopher F
authors.initials: CF
authors.lastname: Thompson
authors.affiliation: Departments of Medicinal Chemistry and Cardiovascular Diseases, Merck Research Laboratories , Rahway, New Jersey 07065, United States.
authors.forename: Amjad
authors.initials: A
authors.lastname: Ali
authors.affiliation: Departments of Medicinal Chemistry and Cardiovascular Diseases, Merck Research Laboratories , Rahway, New Jersey 07065, United States.
authors.forename: Nazia
authors.initials: N
authors.lastname: Quraishi
authors.affiliation: Departments of Medicinal Chemistry and Cardiovascular Diseases, Merck Research Laboratories , Rahway, New Jersey 07065, United States.
authors.forename: Zhijian
authors.initials: Z
authors.lastname: Lu
authors.affiliation: Departments of Medicinal Chemistry and Cardiovascular Diseases, Merck Research Laboratories , Rahway, New Jersey 07065, United States.
authors.forename: Milton L
authors.initials: ML
authors.lastname: Hammond
authors.affiliation: Departments of Medicinal Chemistry and Cardiovascular Diseases, Merck Research Laboratories , Rahway, New Jersey 07065, United States.
authors.forename: Peter J
authors.initials: PJ
authors.lastname: Sinclair
authors.affiliation: Departments of Medicinal Chemistry and Cardiovascular Diseases, Merck Research Laboratories , Rahway, New Jersey 07065, United States.
authors.forename: Matt S
authors.initials: MS
authors.lastname: Anderson
authors.affiliation: Departments of Medicinal Chemistry and Cardiovascular Diseases, Merck Research Laboratories , Rahway, New Jersey 07065, United States.
authors.forename: Suzanne S
authors.initials: SS
authors.lastname: Eveland
authors.affiliation: Departments of Medicinal Chemistry and Cardiovascular Diseases, Merck Research Laboratories , Rahway, New Jersey 07065, United States.
authors.forename: Qiu
authors.initials: Q
authors.lastname: Guo
authors.affiliation: Departments of Medicinal Chemistry and Cardiovascular Diseases, Merck Research Laboratories , Rahway, New Jersey 07065, United States.
authors.forename: Sheryl A
authors.initials: SA
authors.lastname: Hyland
authors.affiliation: Departments of Medicinal Chemistry and Cardiovascular Diseases, Merck Research Laboratories , Rahway, New Jersey 07065, United States.
authors.forename: Denise P
authors.initials: DP
authors.lastname: Milot
authors.affiliation: Departments of Medicinal Chemistry and Cardiovascular Diseases, Merck Research Laboratories , Rahway, New Jersey 07065, United States.
authors.forename: Carl P
authors.initials: CP
authors.lastname: Sparrow
authors.affiliation: Departments of Medicinal Chemistry and Cardiovascular Diseases, Merck Research Laboratories , Rahway, New Jersey 07065, United States.
authors.forename: Samuel D
authors.initials: SD
authors.lastname: Wright
keywords: CETP; Cholesteryl ester transfer protein; HDL; cardiovascular disease; high density lipoprotein; oxazolidinone