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  • Title: Identification of a potent and metabolically stable series of fluorinated diphenylpyridylethanamine-based cholesteryl ester transfer protein inhibitors.
    Author: Miller MM, Liu Y, Jiang J, Johnson JA, Kamau M, Nirschl DS, Wang Y, Harikrishnan L, Taylor DS, Chen AY, Yin X, Seethala R, Peterson TL, Zvyaga T, Zhang J, Huang CS, Wexler RR, Poss MA, Lawrence RM, Adam LP, Salvati ME.
    Journal: Bioorg Med Chem Lett; 2012 Oct 15; 22(20):6503-8. PubMed ID: 22995620.
    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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