The class
New biphenyl oxazolidinone CETP inhibitor scaffold reaches sub-100 nanomolar potency (ACS Med Chem Lett 2011)
Original title: Discovery of substituted biphenyl oxazolidinone inhibitors of cholesteryl ester transfer protein
Building on the rationale that raising HDL-C through CETP inhibition could reduce cardiovascular disease risk, medicinal chemists describe a new class of CETP inhibitors built around an oxazolidinone core. The lead scaffold, a substituted biphenyl oxazolidinone, reaches sub-100 nM potency (IC50 below 100 nM) against cholesteryl ester transfer activity, establishing it as a viable starting point for further optimization within the CETP inhibitor medicinal chemistry landscape of the early 2010s.
Original 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.
Summary written by cetpinhibition.org from the published abstract; figures as published. Page updated 19 August 2026. Methods.