标题:
贝特类调血脂药物的研究进展The New Idea in the Synthesis of Lipid-Regulator Fibrates
作者:
夏莹, 额尔敦, 乌恩
关键字:
高血脂, 贝特类, 合成进展, 活性评价Hyperlipidemia, Fibrates, Synthesis Progress, Activity Evaluation
期刊名称:
《Hans Journal of Medicinal Chemistry》, Vol.2 No.4, 2014-11-18
摘要:
贝特类药物在调血脂领域具有举足轻重的位置，它在降低甘油三酯，高密度脂蛋白，总胆固醇方面具有显著疗效，与临床上应用较多的他汀类药物相比，贝特类药物的不良反应较轻。本综述在对高脂血症和调血脂药物进行介绍的基础上，主要阐述了贝特类调血脂药物的作用机制，说明其优势，对近5年国内外贝特类药物的合成方向及药理活性进行综述，包括全合成的路线优化，结构改造制备双受体激动剂，改善油水分配系数，贝特类药物与具有调血脂活性的天然产物结合等，以期为贝特类的进一步研究提供方向。The lipid-regulating agent fibrate plays an important role in lowering the blood lipid. It can signif-icantly reduce the level of total cholesterol, triglyceride and high-density lipoprotein in blood, and it has less side-effect than the mostly used Statins. In this review, we mainly show the mechanism and advantages of the fibrates, as well as the introduction of the disease high-blood-lipid or the li-pid-regulating agents. We summary the synthesis and pharmacological activities in the past 5 years at home and abroad, including the better routes of its synthesis, changing the construction to get the double-receptor agonist, improving the oil-water partition coefficient and the binding rate in vivo. So we can get the new idea for the further study.