Faculty of Pharmaceutical Sciences, PCTE Group of Institutes, Campus-2, Near Baddowal Cantt. Ferozepur Road, Ludhiana 142021, India; Department of Pharmaceutical Chemistry, School of Pharmaceutical Sciences, Lovely Professional University, Jalandhar-Delhi G.T. Road (NH-1), Phagwara, Punjab 144411, India.
Department of Chemistry, Guru Nanak Dev University College, Patti, Distt. Tarn Taran, India.
Bioorg Med Chem. 2021 Sep 15;46:116354. doi: 10.1016/j.bmc.2021.116354. Epub 2021 Aug 10.
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,在全球范围内日益增多。T2DM 是一种代谢紊乱,其特征是胰岛素缺乏或对胰岛素的抵抗,从而导致血液中的葡萄糖水平升高。有各种方法可以治疗糖尿病,但仍然没有治愈这种疾病的方法。DPP-4 抑制剂是药物发现领域的一个特权靶点,为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而起作用,从而通过最小的副作用降低血糖水平。西他列汀、维格列汀、利格列汀等是世界范围内批准用于治疗糖尿病的不同 DPP-4 类药物。氰基吡咯烷、三唑并哌嗪酰胺、吡咯烷是各种 DPP-4 抑制剂中的基本核心核,具有潜在的作用。在过去的几年中,研究人员已经应用了各种方法来合成有效的 DPP-4 抑制剂作为抗糖尿病药物,而没有体重增加、心血管风险、视网膜病变等副作用。本综述还将强调研究人员为开发 DPP-4 抑制剂而采用的最新策略和原理。本综述还揭示了其他各种方法,如分子建模、基于配体的药物设计、高通量筛选等,被各种研究小组用于开发潜在的 DPP-4 抑制剂。