【摘要】 二肽基肽酶Ⅳ(dipeptidyl peptidaseⅣ,DPP-Ⅳ)是抗2型糖尿病的新靶点之一,其抑制剂的研发已经成为当今抗糖尿病药物研究的热点,其中拟肽类DPP-Ⅳ抑制剂是一重要类型,此类抑制剂的研究最为深入和广泛,代表药物维格列汀(vildagliptin)和沙格列汀(saxagliptin)均已进入市场。本文从拟肽类DPP-Ⅳ抑制剂的发现过程、优化策略及构效关系等方面综述近年来该类抑制剂的研究进展。更多还原

【Abstract】 Dipeptidyl peptidase Ⅳ(DPP-Ⅳ) is one of the new targets for the treatment of type 2 diabetes mellitus,and its inhibitors have become the research hotspot in recent years.The peptidomimetic inhibitors as an important class have been studied extensively and deeply.The representative compounds vildagliptin and saxagliptin have been approved for marketing.Herein,the recent advances in peptidomimetic DPP-Ⅳ inhibitors were summarized with emphasis on the process of their discovery,optimization and discussion of structure-activity relationships.更多还原