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  • Title: Biphenyl-substituted oxazolidinones as cholesteryl ester transfer protein inhibitors: modifications of the oxazolidinone ring leading to the discovery of anacetrapib.
    Author: Smith CJ, Ali A, Hammond ML, Li H, Lu Z, Napolitano J, Taylor GE, Thompson CF, Anderson MS, Chen Y, Eveland SS, Guo Q, Hyland SA, Milot DP, Sparrow CP, Wright SD, Cumiskey AM, Latham M, Peterson LB, Rosa R, Pivnichny JV, Tong X, Xu SS, Sinclair PJ.
    Journal: J Med Chem; 2011 Jul 14; 54(13):4880-95. PubMed ID: 21682257.
    Abstract:
    The development of the structure-activity studies leading to the discovery of anacetrapib is described. These studies focused on varying the substitution of the oxazolidinone ring of the 5-aryloxazolidinone system. Specifically, it was found that substitution of the 4-position with a methyl group with the cis-stereochemistry relative to the 5-aryl group afforded compounds with increased cholesteryl ester transfer protein (CETP) inhibition potency and a robust in vivo effect on increasing HDL-C levels in transgenic mice expressing cynomolgus monkey CETP.
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