2-Arylbenzoxazoles as CETP inhibitors: Raising HDL-C in cynoCETP transgenic mice

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• 作者：Florida Kallashi ; Dooseop Kim ; Jennifer Kowalchick ; You Jung Park ; Julianne A. Hunt ; Amjad Ali ; Cameron J. Smith ; Milton L. Hammond ; James V. Pivnichny ; Xinchun Tong ; Suoyu S. Xu ; Matt S. Anderson ; Yi
• 关键词：CETP ; Cholesteryl ester transfer protein ; HDL-C ; CVD ; 2-Arylbenzoxazole
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2011
• 出版时间：1 January 2011
• 年：2011
• 卷：21
• 期：1
• 页码：558-561
• 全文大小：906 K

文摘

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.