Discovery of substituted biphenyl oxazolidinone inhibitors of cholesteryl ester transfer protein.

ACS Med Chem Lett

Departments of Medicinal Chemistry and Cardiovascular Diseases, Merck Research Laboratories , Rahway, New Jersey 07065, United States.

Published: June 2011

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.

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4018150PMC
http://dx.doi.org/10.1021/ml100309nDOI Listing

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