Discovery of Substituted Biphenyl Oxazolidinone Inhibitors of

Mar 24, 2011 - (13) In fact, treatment with torcetrapib increased the risk of death from both ... Surprisingly, the oxazolidinone does not have the su...
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LETTER pubs.acs.org/acsmedchemlett

Discovery of Substituted Biphenyl Oxazolidinone Inhibitors of Cholesteryl Ester Transfer Protein Christopher F. Thompson,*,† Amjad Ali,† Nazia Quraishi,† Zhijian Lu,† Milton L. Hammond,† Peter J. Sinclair,† Matt S. Anderson,‡ Suzanne S. Eveland,‡ Qiu Guo,‡ Sheryl A. Hyland,‡ Denise P. Milot,‡ Carl P. Sparrow,‡ and Samuel D. Wright‡ Departments of †Medicinal Chemistry and ‡Cardiovascular Diseases, Merck Research Laboratories, Rahway, New Jersey 07065, United States

bS Supporting Information 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 (