Thompson Christopher F, Ali Amjad, Quraishi Nazia, Lu Zhijian, Hammond Milton L, Sinclair Peter J, Anderson Matt S, Eveland Suzanne S, Guo Qiu, Hyland Sheryl A, Milot Denise P, Sparrow Carl P, Wright Samuel D
Departments of Medicinal Chemistry and Cardiovascular Diseases, Merck Research Laboratories , Rahway, New Jersey 07065, United States.
ACS Med Chem Lett. 2011 Mar 24;2(6):424-7. doi: 10.1021/ml100309n. eCollection 2011 Jun 9.
Recently, there has been a strong interest in the ability to increase levels of high density lipoprotein-cholesterol (HDL-C). This interest stems from the hypothesis that such an elevation in HDL-C will decrease the likelihood of cardiovascular disease. Inhibition of cholesteryl ester transfer protein (CETP) has been shown to elevate HDL-C levels in human subjects. This letter describes the discovery of a novel and potent (<100 nM IC50 for the inhibition of CE transfer) CETP inhibitor scaffold containing an oxazolidinone core.
最近，人们对提高高密度脂蛋白胆固醇（HDL-C）水平的能力产生了浓厚兴趣。这种兴趣源于这样一种假设，即HDL-C的这种升高将降低心血管疾病的可能性。已证明抑制胆固醇酯转移蛋白（CETP）可提高人体受试者的HDL-C水平。这封信描述了一种新型强效（抑制CE转移的IC50<100 nM）CETP抑制剂支架的发现，该支架含有恶唑烷酮核心。
