Fluorinated diphenylpyridylethanamine derivatives balance metabolic stability and CETP potency (Bioorg Med Chem Lett 2012)

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

Bioorg Med Chem Lett · 9 August 2012 · 4

Miller MM, Liu Y, Jiang J, Johnson JA, Kamau M, Nirschl DS, Wang Y, Harikrishnan L, Taylor DS, Chen AY, Yin X, Seethala R et al.

Researchers describe a novel series of diphenylpyridylethanamine-based cholesteryl ester transfer protein (CETP) inhibitors. Optimisation focused on the urea moiety of the compounds, particularly through incorporation of fluorine, to balance in vitro metabolic stability against CETP inhibitory potency measured in a whole-plasma assay. The work identifies a metabolically stable, potent series of CETP inhibitors as candidates for further development.

Original 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.

Summary written by cetpinhibition.org from the published abstract; figures as published. Page updated 19 August 2026. Methods.