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  • Title: 2-Arylbenzoxazoles as CETP inhibitors: raising HDL-C in cynoCETP transgenic mice.
    Author: Kallashi F, Kim D, Kowalchick J, Park YJ, Hunt JA, Ali A, Smith CJ, Hammond ML, Pivnichny JV, Tong X, Xu SS, Anderson MS, Chen Y, Eveland SS, Guo Q, Hyland SA, Milot DP, Cumiskey AM, Latham M, Peterson LB, Rosa R, Sparrow CP, Wright SD, Sinclair PJ.
    Journal: Bioorg Med Chem Lett; 2011 Jan 01; 21(1):558-61. PubMed ID: 21094047.
    Abstract:
    We describe structure-activity studies leading to the discovery of 2-arylbenzoxazole 3, the first in a series to raise serum high-density lipoprotein cholesterol levels in transgenic mice. Replacement of the 4-piperidinyloxy moiety with piperazinyl provided a more synthetically tractable lead, which upon optimization resulted in compound 4, an excellent inhibitor of cholesteryl ester transfer protein function with good pharmacokinetic properties and in vivo efficacy.
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