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。 Dipeptidyl peptidase Ⅳ (DPP-Ⅳ) is one of the new anti-type 2 diabetes targets. The development of its inhibitors has become a hot research topic in the field of antidiabetic drugs. Peptoid DPP-Ⅳ inhibitors Is one of the most important types. The most extensive and extensive research on these inhibitors has been made. The representative drugs vildagliptin and saxagliptin have entered the market. In this paper, we review the recent progress in the discovery of DPP-IV inhibitors, optimization strategies and their structure-activity relationship.