Identification of a potent and metabolically stable series of fluorinated diphenylpyridylethanamine-based cholesteryl ester transfer protein inhibitors

doi:10.1016/j.bmcl.2012.08.011

Bioorganic & Medicinal Chemistry Letters

Volume 22, Issue 20, 15 October 2012, Pages 6503-6508

https://doi.org/10.1016/j.bmcl.2012.08.011 Get rights and content

Abstract

A novel series of diphenylpyridylethanamine-based inhibitors of cholesteryl ester transfer protein is described. Optimization of the urea moiety, particularly by incorporation of fluorine, is explored to balance in vitro metabolic stability with CETP potency in the whole plasma assay.

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Identification of a potent and metabolically stable series of fluorinated diphenylpyridylethanamine-based cholesteryl ester transfer protein inhibitors

Abstract

Graphical abstract

Circulation

Am. J. Cardiol.

J. Lipid Res.

Arterioscler. Thromb. Vasc. Biol.

Curr. Opin. Drug Discovery Dev.

Annu. Rep. Med. Chem.

Lipid Res.

J. Biol. Chem.

Nature

J. Med. Chem.

Atherosclerosis

J. Med. Chem.

Engl. J. Med.

J. Amer. Med. Assoc.

Lancet

Tetrahedron

Arterioscler. Thromb. Vasc. Biol.

N. Engl J. Med.

JAMA

Lancet

Engl. J. Med.

Engl. J. Med.

Am. J. Med.

J. Am. Med. Assoc.

Am. J. Cardiol.

Atherosclerosis

JAMA

JAMA

Am. J. Med.

Curr. Med. Res. Opin.

Eur. Heart J. Suppl.

Annu. Rev. Pharmacol. Toxicol.

J. Am. Coll. Cardiol.