Petrov Valentin, Aleksandrova Teodora, Pashev Aleksandar
Department of Chemistry and Biochemistry, Faculty of Pharmacy, Medical University-Pleven, 1 St. Kliment Ohridski Str., 5800 Pleven, Bulgaria.
Molecules. 2025 Feb 25;30(5):1043. doi: 10.3390/molecules30051043.
Dipeptidyl peptidase IV (DPP-IV) is a serine protease whose inhibition has been an object of considerable interest in the context of developing novel treatments for type 2 diabetes mellitus. The development of novel DPP-IV inhibitors from natural or synthetic origin has seen a growing scientific interest in recent years, especially during the SARS-CoV-2 pandemic, when DPP-IV inhibitors were found to be of beneficial therapeutic value for COVID-19 patients. The present manuscript aims to summarize the most recent information on the synthesis of different DPP-IV inhibitors, emphasizing the various heterocyclic scaffolds that can be found in them. Special attention is devoted to DPP-IV inhibitors that are currently in clinical trials. Different synthetic approaches for the construction of DPP-IV inhibitors are discussed, as well as the most recent developments in the field.
二肽基肽酶IV(DPP-IV)是一种丝氨酸蛋白酶,在开发2型糖尿病新疗法的背景下,其抑制作用一直是人们相当感兴趣的对象。近年来,从天然或合成来源开发新型DPP-IV抑制剂引发了越来越多的科学关注,尤其是在严重急性呼吸综合征冠状病毒2(SARS-CoV-2)大流行期间,当时发现DPP-IV抑制剂对2019冠状病毒病(COVID-19)患者具有有益的治疗价值。本手稿旨在总结不同DPP-IV抑制剂合成的最新信息,强调其中可发现的各种杂环骨架。特别关注目前正在进行临床试验的DPP-IV抑制剂。讨论了构建DPP-IV抑制剂的不同合成方法以及该领域的最新进展。