Department of Medicinal Chemistry, Merck Research Laboratories, Rahway NJ 07065, United States.
Bioorg Med Chem Lett. 2010 Jan 1;20(1):346-9. doi: 10.1016/j.bmcl.2009.10.099. Epub 2009 Oct 29.
A series of 2-arylbenzoxazole inhibitors of the cholesterol ester transfer protein (CETP) is described. Structure-activity studies focused on variation of the substitution of the benzoxazole moiety. Substitution at the 5- and 7-positions of the benzoxazole moiety was found to be beneficial for CETP inhibition. Compound 47 was found to be the most potent inhibitor in this series and inhibited CETP with an IC(50) of 28nM.
本文描述了一系列胆固醇酯转移蛋白（CETP）的 2-芳基苯并恶唑抑制剂。构效关系研究主要集中在苯并恶唑部分取代基的变化上。苯并恶唑部分的 5-位和 7-位取代被发现有利于 CETP 抑制。化合物 47 被发现是该系列中最有效的抑制剂，对 CETP 的抑制作用的 IC50 为 28nM。
