Department of Chemistry, Quaid-i-Azam University, Islamabad, Pakistan.
H. E. J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi, Pakistan.
Expert Opin Ther Pat. 2022 Sep;32(9):969-1001. doi: 10.1080/13543776.2022.2116312. Epub 2022 Sep 6.
Oxadiazole is a unique class of heterocycle, possessing numerous important biomedical and therapeutic applications, such as anti-bacterial, anti-cancer, anti-inflammatory, inhibitors for diverse enzymes, receptor modulators, and neuroprotective properties. The rapid development in the field of oxadiazole-containing structures is confirmed by the development of numerous clinical drugs, such as doxazosin, nesapidil, pleconaril, fasiplon, ataluren, zibotentan, and prenoxdiazine as selected examples.
This review provides a comprehensive overview of the range of biological applications of oxadiazole-containing drugs in a range of patents from 2013 to 2021. The information was collected from available data sources including SciFinder, Reaxys, MedLine, and Chemical Abstracts.
Oxadiazole is an established class of compounds with fascinating biological properties. The importance of oxadiazoles can be recognized by their enormous application in a wide spectrum of medicinal chemistry from anticancer, lantibiotics, and antidiabetics to their use in agriculture and neuroprotection. For instance, the oxadiazole-based compounds have shown the ability to modulate a variety of receptors including the M4 receptor agonists, S1P1 receptor modulators, SSTR5 antagonists, orexin type-2 receptor agonists, liver X receptor agonists, and many more. This testifies to the special features associated with the oxadiazole scaffold, making it a significant pharmacophore.
恶二唑是一类独特的杂环，具有许多重要的生物医学和治疗应用，如抗菌、抗癌、抗炎、多种酶抑制剂、受体调节剂和神经保护特性。含有恶二唑结构的化合物领域的快速发展得到了许多临床药物的证实，如多沙唑嗪、奈西立肽、普乐可复、法西洛朋、阿特伦、齐伯坦和苯并恶嗪等。
本综述提供了 2013 年至 2021 年专利中含恶二唑药物的广泛生物应用的全面概述。这些信息是从可用的数据源收集的，包括 SciFinder、Reaxys、MedLine 和 Chemical Abstracts。
恶二唑是一类具有迷人生物学性质的已建立的化合物。恶二唑的重要性可以从它们在广泛的药物化学中的应用中得到认可，从抗癌、类抗生素和抗糖尿病到在农业和神经保护中的应用。例如，基于恶二唑的化合物已显示出调节多种受体的能力，包括 M4 受体激动剂、S1P1 受体调节剂、SSTR5 拮抗剂、食欲素 2 型受体激动剂、肝 X 受体激动剂等。这证明了恶二唑支架相关的特殊特征，使其成为一个重要的药效团。
