2-(4-Carbonylphenyl)benzoxazole inhibitors of CETP: Attenuation of hERG binding and improved HDLc-raising efficacy

Ramzi F. Sweis,Julianne A. Hunt,Peter J. Sinclair,Ying Chen,Suzanne S. Eveland,Qiu Guo,Sheryl A. Hyland,Denise P. Milot,Anne-Marie Cumiskey,Melanie Latham,Raymond Rosa,Larry Peterson,Carl P. Sparrow,Matt S. Anderson

Bioorganic & Medicinal Chemistry Letters（2011）

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摘要

Compounds 7e and 7f were the first in this series of benzoxazoles found to be a potent inhibitors of CETP (IC50=22 and 18nM), with robust in vivo efficacy (ΔHDLc=33 and 27mg/dL) and absent of any hERG binding liabilities.

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关键词

Cholesteryl ester transfer protein,Cholesterol,hERG,HDLc,LDLc,Atherosclerosis

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