Department of Pharmaceutical Chemistry, G R T Institute of Pharmaceutical Education and Research, GRT Mahalakshmi Nagar, Tiruttani 631209, Tamil Nadu, India.
Department of Pharmaceutical Chemistry, Y. B. Chavan College of Pharmacy, Aurangabad 431001, Maharashtra, India.
Molecules. 2022 Sep 15;27(18):6001. doi: 10.3390/molecules27186001.
Dipeptidyl peptidase-IV (DPP-IV) inhibitors, often known as gliptins, have been used to treat type 2 diabetes mellitus (T2DM). They may be combined with other medications as an additional treatment or used alone as a monotherapy. In addition to insulin, sulfonylureas, thiazolidinediones, and metformin, these molecules appear as possible therapeutic options. Oxadiazole rings have been employed in numerous different ways during drug development efforts. It has been shown that including them in the pharmacophore increases the amount of ligand that may be bound. The exceptional hydrogen bond acceptor properties of oxadiazoles and the distinct hydrocarbon bonding potential of their regioisomers have been established. Beside their anti-diabetic effects, oxadiazoles display a wide range of pharmacological properties. In this study, we made the assumption that molecules containing oxadiazole rings may afford a different approach to the treatment of diabetes, not only for controlling glycemic levels but also for preventing atherosclerosis progression and other complications associated with diabetes. It was observed that oxadiazole fusion with benzothiazole, 5-(2,5,2-trifluoroethoxy) phenyl, β-homophenylalanine, 2-methyl-2-{5-(4-chlorophenyl), diamine-bridged -coumarinyl, 5-aryl-2-(6'-nitrobenzofuran-2'-yl), nitrobenzofuran, and/or oxindole leads to potential anti-diabetic activity.
二肽基肽酶-4(DPP-4)抑制剂,通常称为gliptins,已被用于治疗 2 型糖尿病(T2DM)。它们可以与其他药物联合使用作为附加治疗,也可以单独作为单一疗法使用。除了胰岛素、磺酰脲类、噻唑烷二酮类和二甲双胍外,这些分子似乎是潜在的治疗选择。在药物开发过程中,已采用了多种不同的方法来使用恶二唑环。研究表明,在药效团中加入它们可以增加可能结合的配体数量。恶二唑具有独特的氢键受体性质,其区域异构体具有独特的烃键合潜力。除了抗糖尿病作用外,恶二唑还表现出广泛的药理特性。在这项研究中,我们假设含有恶二唑环的分子可能为治疗糖尿病提供一种不同的方法,不仅可以控制血糖水平,还可以预防动脉粥样硬化进展和其他与糖尿病相关的并发症。研究观察到,恶二唑与苯并噻唑、5-(2,5,2-三氟乙氧基)苯基、β-高苯丙氨酸、2-甲基-2-{5-(4-氯苯基)、二胺桥接-香豆素基、5-芳基-2-(6'-硝基苯并呋喃-2'-基)、硝基苯并呋喃和/或吲哚恶二唑的融合导致潜在的抗糖尿病活性。