环氧合酶-2和5-脂氧化酶双重抑制剂的研究进展

Advances in the Research on the Cyclooxygenase-2 and 5-Lipoxygenase Dual Inhibitors

传统的非甾体抗炎药和选择性环氧合酶-2(COX-2)抑制剂在治疗炎症过程中引发胃肠道及肾脏不良反应,制约了其临床应用。COX-2和5-脂氧化酶(5-LOX)双重抑制剂同时抑制前列腺素(PGs)和炎症介质白三烯类(LTs)的生物合成,比单一的抑制剂抗炎效果好、安全性高,是一类有发展前景的新型非甾体抗炎药。笔者简要介绍COX-2/5-LOX双重抑制剂的研究进展,并讨论其作用机制及构效关系。

Classical Non-Steroidal Anti-Inflammatory Drugs（NSAIDs） and selective Cyclooxygenase-2 （COX-2） inhibitors present GI damage and diverse side effects for the treatment of inflammatory disease, which limited their clinical development. These compounds with equal capabilities of inhibiting COX-2 and（5-1ipoxygenase,5-LOX） are expected to be more safe and efficient for NSAIDs. In this paper, the molecular basis, structure-activity relationships （SAR） as well as various structural families of the dual COX-2and 5- LOX inhibitors are reviewed.