Clader John W
Department of Cardiovascular and CNS Medicinal Chemistry, Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033-1300, USA.
Curr Top Med Chem. 2005;5(3):243-56. doi: 10.2174/1568026053544498.
Atherosclerotic coronary artery disease remains a major healthcare concern especially in developed countries. While lowering plasma cholesterol levels via diet, exercise, and pharmacotherapy can reduce this risk of developing coronary artery disease, there remains a need for more effective drug therapies. The azetidinone cholesterol absorption inhibitors typified by ezetimibe represent the first new approach to lipid lowering therapy in more than a decade. This review summarizes the medicinal chemistry of the azetidinone cholesterol absorption inhibitors as a class, with emphasis on factors that contributed both to the discovery of ezetimibe as well as to our overall understanding of S.A.R. trends in this area.
动脉粥样硬化性冠状动脉疾病仍然是一个主要的医疗问题，尤其是在发达国家。虽然通过饮食、运动和药物治疗降低血浆胆固醇水平可以降低患冠状动脉疾病的风险，但仍需要更有效的药物治疗。以依折麦布为代表的氮杂环丁酮类胆固醇吸收抑制剂是十多年来第一种新的降脂治疗方法。本综述总结了氮杂环丁酮类胆固醇吸收抑制剂这一类药物的药物化学，重点关注促成依折麦布发现的因素以及我们对该领域构效关系趋势的整体理解。
