Department of Chemistry, Quaid-i-Azam University, Islamabad, 45320, Pakistan.
Department of Chemistry, Quaid-i-Azam University, Islamabad, 45320, Pakistan.
Eur J Med Chem. 2023 Mar 5;249:115119. doi: 10.1016/j.ejmech.2023.115119. Epub 2023 Jan 17.
Diabetes mellitus is one of the biggest challenges for the scientific community in the 21st century. It is a well-recognized multifactorial health problem contributes significantly to high mortality rates by causing serious health complications mainly related to cardiovascular diseases, kidney damage and neuropathy. The inhibition of α-glucosidase (enzyme that catalyses starch hydrolysis in the intestine) is an effective therapeutic approach for controlling hyperglycemia associated with type-2 diabetes. However, the presently approved drugs/inhibitors such as acarbose, miglitol and voglibose have several undesirable gastrointestinal side effects impeding their applications. Therefore, search for novel and more effective inhibitors with reduced side effects and less cost remains a fascinating area of research. In this context, a large variety of α-glucosidase inhibitors have been identified in recent years that demands attention from drug development community. This review is therefore an effort to summarize and highlight the promising α-glucosidase inhibitors especially those which are primarily based on aromatic heterocyclic scaffolds such as coumarin, imidazole, isatin, pyrimidine, quinazoline, triazine, thiazole etc, having improved safety and pharmacological profiles.
糖尿病是 21 世纪科学界面临的最大挑战之一。它是一个公认的多因素健康问题，通过引起严重的健康并发症，主要与心血管疾病、肾脏损害和神经病变，对高死亡率有重大影响。抑制α-葡萄糖苷酶（在肠道中催化淀粉水解的酶）是控制与 2 型糖尿病相关的高血糖的有效治疗方法。然而，目前批准的药物/抑制剂，如阿卡波糖、米格列醇和伏格列波糖，具有多种不良的胃肠道副作用，阻碍了它们的应用。因此，寻找具有降低副作用和成本的新型、更有效的抑制剂仍然是一个引人关注的研究领域。在这方面，近年来已经发现了大量的α-葡萄糖苷酶抑制剂，这引起了药物开发界的关注。因此，本文综述强调了有前途的α-葡萄糖苷酶抑制剂，特别是那些主要基于芳香杂环骨架的抑制剂，如香豆素、咪唑、靛红、嘧啶、喹唑啉、三嗪、噻唑等，它们具有改善的安全性和药理学特性。
