Buravchenko Galina I, Shchekotikhin Andrey E
Gause Institute of New Antibiotics, 119021 Moscow, Russia.
Pharmaceuticals (Basel). 2023 Aug 17;16(8):1174. doi: 10.3390/ph16081174.
-Oxides of heterocyclic compounds are the focus of medical chemistry due to their diverse biological properties. The high reactivity and tendency to undergo various rearrangements have piqued the interest of synthetic chemists in heterocycles with -oxide fragments. Quinoxaline 1,4-dioxides are an example of an important class of heterocyclic -oxides, whose wide range of biological activity determines the prospects of their practical use in the development of drugs of various pharmaceutical groups. Derivatives from this series have found application in the clinic as antibacterial drugs and are used in agriculture. Quinoxaline 1,4-dioxides present a promising class for the development of new drugs targeting bacterial infections, oncological diseases, malaria, trypanosomiasis, leishmaniasis, and amoebiasis. The review considers the most important methods for the synthesis and key directions in the chemical modification of quinoxaline 1,4-dioxide derivatives, analyzes their biological properties, and evaluates the prospects for the practical application of the most interesting compounds.
杂环化合物的氧化物因其多样的生物学特性而成为药物化学的研究重点。其高反应活性以及易于发生各种重排的倾向激发了合成化学家对含有氧化物片段杂环化合物的兴趣。喹喔啉1,4 -二氧化物是一类重要的杂环氧化物的实例,其广泛的生物活性决定了它们在各类药物研发中实际应用的前景。该系列衍生物已在临床上作为抗菌药物使用,并应用于农业领域。喹喔啉1,4 -二氧化物是开发针对细菌感染、肿瘤疾病、疟疾、锥虫病、利什曼病和阿米巴病的新药的一个有前景的类别。本综述探讨了喹喔啉1,4 -二氧化物衍生物合成的最重要方法及其化学修饰的关键方向,分析了它们的生物学特性,并评估了最具吸引力化合物的实际应用前景。