2-Arylbenzoxazoles as CETP inhibitors: Substitution and modification of the α-alkoxyamide moiety

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• 作者：Julianne A. Hunt ; Silvia Gonzalez ; Florida Kallashi ; Milton L. Hammond ; James V. Pivnichny ; Xinchun Tong ; Suoyu S. Xu ; Matt S. Anderson ; Ying Chen ; Suzanne S. Evel ; Qiu Guo ; Sheryl A. Hyl ; Denise P.
• 关键词：CETP ; Cholesteryl ester transfer protein ; High-density lipoprotein cholesterol ; Low-density lipoprotien cholesterol ; Reverse cholesterol transport ; 2-Arylbenzoxazole
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2010
• 出版时间：1 February 2010
• 年：2010
• 卷：20
• 期：3
• 页码：1019-1022
• 全文大小：1250 K

文摘

The development of a series of 2-arylbenzoxazole α-alkoxyamide and β-alkoxyamine inhibitors of cholesteryl ester transfer protein (CETP) is described. Highly fluorinated α-alkoxyamides proved to be potent inhibitors of CETP in vitro, and the highly fluorinated 2-arylbenzoxazole β-alkoxyamine 4 showed a desirable combination of in vitro potency (IC₅₀ = 151 nM) and oral bioavailability in the mouse.