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1,3,4-Oxadiazole Scaffold in Antidiabetic Drug Discovery: An Overview
Mini-Reviews in Medicinal Chemistry ( IF 3.3 ) Pub Date : 2024-04-22 , DOI: 10.2174/0113895575298181240410041029
Ojasvi Gupta 1 , Gita Chawla 1 , Tathagata Pradhan 1
Affiliation  

:: Diabetes mellitus is one of the biggest challenges for the scientific community in the 21st century. With the increasing number of cases of diabetes and drug-resistant diabetes, there is an urgent need to develop new potent molecules capable of combating this cruel disease. Medicinal chemistry concerns the discovery, development, identification, and interpretation of the mode of action of biologically active compounds at the molecular level. Oxadiazole-based derivatives have come up as a potential option for antidiabetic drug research. Oxadiazole is a five-membered heterocyclic organic compound containing two nitrogen atoms and one oxygen atom in its ring. Oxadiazole hybrids have shown the ability to improve glucose tolerance, enhance insulin sensitivity, and reduce fasting blood glucose levels. The mechanisms underlying the antidiabetic effects of oxadiazole involve the modulation of molecular targets such as peroxisome proliferator-activated receptor gamma (PPARγ), α-glucosidase, α-amylase and GSK-3β which regulate glucose metabolism and insulin secretion. The present review article describes the chemical structure and properties of oxadiazoles and highlights the antidiabetic activity through action on different targets. The SAR for the oxadiazole hybrids has been discussed in this article, which will pave the way for the design and development of new 1,3,4-oxadiazole derivatives as promising antidiabetic agents in the future. We expect that this article will provide comprehensive knowledge and current innovation on oxadiazole derivatives with antidiabetic potential and will fulfil the needs of the scientific community in designing and developing efficacious antidiabetic agents.

中文翻译:

抗糖尿病药物发现中的 1,3,4-恶二唑支架:概述

* 糖尿病是21世纪科学界面临的最大挑战之一。随着糖尿病和耐药糖尿病病例的不断增加,迫切需要开发能够对抗这种残酷疾病的新的有效分子。药物化学涉及分子水平上生物活性化合物的作用模式的发现、开发、鉴定和解释。基于恶二唑的衍生物已成为抗糖尿病药物研究的潜在选择。恶二唑是一种环上含有两个氮原子和一个氧原子的五元杂环有机化合物。恶二唑杂种已显示出改善葡萄糖耐量、增强胰岛素敏感性和降低空腹血糖水平的能力。恶二唑抗糖尿病作用的机制涉及分子靶标的调节,例如过氧化物酶体增殖物激活受体γ (PPARγ)、α-葡萄糖苷酶、α-淀粉酶和 GSK-3β,调节葡萄糖代谢和胰岛素分泌。本综述文章描述了恶二唑的化学结构和性质,并强调了通过作用于不同靶点的抗糖尿病活性。本文讨论了恶二唑杂化物的 SAR,这将为设计和开发新的 1,3,4-恶二唑衍生物作为未来有前景的抗糖尿病药物铺平道路。我们期望本文能够提供具有抗糖尿病潜力的恶二唑衍生物的全面知识和最新创新,并满足科学界设计和开发有效抗糖尿病药物的需求。
更新日期:2024-04-22
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