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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.

SUBMITTER: Thompson CF 

PROVIDER: S-EPMC4018150 | biostudies-literature | 2011 Jun

REPOSITORIES: biostudies-literature

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

Thompson Christopher F CF   Ali Amjad A   Quraishi Nazia N   Lu Zhijian Z   Hammond Milton L ML   Sinclair Peter J PJ   Anderson Matt S MS   Eveland Suzanne S SS   Guo Qiu Q   Hyland Sheryl A SA   Milot Denise P DP   Sparrow Carl P CP   Wright Samuel D SD  

ACS medicinal chemistry letters 20110324 6

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 c  ...[more]

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