Type 2 Diabetes Mellitus (T2DM) is one of the highly prevalence disorder and increasing day by day worldwidely. T2DM is a metabolic disorder, which is characterized by deficiency in insulin or resistance to insulin and thus increases the glucose levels in the blood. Various approaches are there to treat diabetes but still there is no cure for this disease. DPP-4 inhibitor is a privileged target in the field of drug discovery and provides various opportunities in exploring this target for development of molecules as antidiabetic agents. DPP-4 acts by inhibiting the incretin action and thus decreases the level of blood glucose by imparting minimal side effects. Sitagliptin, vildagliptin, linagliptin etc. are the different DPP-4 based drugs approved throughout the world for the treatment of diabetes mellitus. Cyanopyrrolidines, triazolopiperazine amide, pyrrolidines are basic core nucleus present in various DPP-4 inhibitors and has potential effects. In the past few years, researchers had applied various approaches to synthesize potent DPP-4 inhibitors as antidiabetic agent without side effects like weight gain, cardiovascular risks, retinopathy etc. This review will also emphasize the recent strategies and rationale utilized by researchers for the development of DPP-4 inhibitors. This review also reveals about the various other approaches like molecular modelling, ligand based drug designing, high throughput screening etc. are used by the various research group for the development of potential DPP-4 inhibitors.

2 型糖尿病 (T2DM) 是一种高度流行的疾病，并且在全球范围内日益增加。T2DM 是一种代谢紊乱，其特征是胰岛素缺乏或胰岛素抵抗，从而增加血液中的葡萄糖水平。有多种方法可以治疗糖尿病，但仍然无法治愈这种疾病。DPP-4 抑制剂是药物发现领域的一个特权目标，并为探索该目标以开发作为抗糖尿病药物的分子提供了各种机会。DPP-4 通过抑制肠促胰岛素作用起作用，从而通过赋予最小的副作用来降低血糖水平。西格列汀、维格列汀、利格列汀等是世界各地批准用于治疗糖尿病的不同的基于 DPP-4 的药物。氰基吡咯烷，三唑并哌嗪酰胺、吡咯烷是各种 DPP-4 抑制剂中存在的基本核心核，具有潜在作用。在过去的几年里，研究人员应用各种方法来合成有效的 DPP-4 抑制剂作为抗糖尿病药物，没有副作用，如体重增加、心血管风险、视网膜病变等。本综述还将强调研究人员最近使用的开发策略和基本原理DPP-4 抑制剂。这篇综述还揭示了各种其他方法，如分子建模、基于配体的药物设计、高通量筛选等，被各个研究小组用于开发潜在的 DPP-4 抑制剂。研究人员已经应用各种方法来合成有效的 DPP-4 抑制剂作为抗糖尿病药物，没有副作用，如体重增加、心血管风险、视网膜病变等。本综述还将强调研究人员最近用于开发 DPP-4 抑制剂的策略和基本原理。这篇综述还揭示了各种其他方法，如分子建模、基于配体的药物设计、高通量筛选等，被各个研究小组用于开发潜在的 DPP-4 抑制剂。研究人员已经应用各种方法来合成有效的 DPP-4 抑制剂作为抗糖尿病药物，没有副作用，如体重增加、心血管风险、视网膜病变等。本综述还将强调研究人员最近用于开发 DPP-4 抑制剂的策略和基本原理。这篇综述还揭示了各种其他方法，如分子建模、基于配体的药物设计、高通量筛选等，被各个研究小组用于开发潜在的 DPP-4 抑制剂。