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Synthetic Protocols and Applications of 1,2,5-Oxadiazoles: A Review
Letters in Organic Chemistry ( IF 0.7 ) Pub Date : 2023-09-21 , DOI: 10.2174/1570178620666230905145050
Greesh Kumar 1 , Rajnish Kumar 1 , Avijit Mazumder 1 , Salahuddin Salahuddin 1 , Upendra Kumar 1
Affiliation  

The 1,2,5-oxadiazole framework has garnered a lot of interest among many nitrogen heterocycles because of its capacity to give off NO under physiological circumstances. Because of this, major efforts by chemical scientists have been made to create novel drug possibilities in medicinal, material, and agriculture science that include the NO-donor 1,2,5-oxadiazole N-oxide subunit coupled to a known drug or a possible pharmacophore by C-C/C-N links or by using a suitable spacer. In the last few years, 1,2,5-oxadiazole and its derivatives have been reported as good pharmacophores as carbonic anhydrase inhibitors, antibacterial, vasodilating agents, antimalarial, anticancer, etc. In the presented manuscript, we reviewed granted patents (last 10 years), different synthetic strategies (last 27 years) of 1,2,5- oxadiazoles and their N-oxide derivatives synthesis such as cycloaddition, dimerization, cyclodehydration, condensation, thermolysis, nitration, oxidation, ring-conversion, etc. These synthetic methods have also been analyzed for their merits and demerits. The manuscript also highlighted various applications of 1,2,5-oxadiazole and its derivatives. We hope that researchers across the scientific streams will benefit from the presented review articles for designing their work related to 1,2,5-oxadiazoles.

中文翻译:

1,2,5-恶二唑的合成方案和应用:综述

1,2,5-恶二唑骨架由于其在生理环境下释放NO的能力而在许多氮杂环中引起了人们的广泛兴趣。因此,化学科学家们做出了巨大的努力,以在医学、材料和农业科学领域创造新的药物可能性,其中包括与已知药物或可能的药物偶联的 NO 供体 1,2,5-恶二唑 N-氧化物亚基。药效团通过 CC/CN 连接或使用合适的间隔基。在过去的几年中,1,2,5-恶二唑及其衍生物已被报道为良好的药效团,如碳酸酐酶抑制剂、抗菌剂、血管舒张剂、抗疟药、抗癌药等。在本手稿中,我们回顾了已授权的专利(最近 10 项)年),1,2,5-恶二唑及其N-氧化物衍生物合成的不同合成策略(最近27年),如环加成、二聚、环脱水、缩合、热解、硝化、氧化、环化等。这些合成还分析了各种方法的优缺点。该手稿还强调了 1,2,5-恶二唑及其衍生物的各种应用。我们希望各科学领域的研究人员能够从所提交的综述文章中受益,以设计与 1,2,5-恶二唑相关的工作。
更新日期:2023-09-21
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