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  • Title: Discovery of hydroxyl 1,2-diphenylethanamine analogs as potent cholesterol ester transfer protein inhibitors.
    Author: Jiang J, Finlay H, Johnson JA, Harikrishnan L, Kamau M, Qiao J, Wang T, Adam L, Taylor D, Yang R, Sleph P, Chen AYA, Yin X, Wexler R, Salvati ME.
    Journal: Bioorg Med Chem Lett; 2016 Jul 15; 26(14):3278-3281. PubMed ID: 27256912.
    Abstract:
    Hydroxyl 1,2-diphenylethanamine analogs were identified as potent inhibitors of cholesterol ester transfer protein (CETP), a therapeutic target to raise HDL cholesterol. In an effort to improve the pharmaceutical properties in the previously disclosed DiPhenylPyridineEthanamine (DPPE) series, polar groups were introduced to the N-linked quaternary center. Optimization of analogues for potency, in vitro liability profile and efficacy led to identification of lead compound 16 which demonstrated robust pharmacodynamic effects in human CETP/apo-B100 dual transgenic mice.
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