Review on the potential of 1,3,4-Oxadiazine derivatives: Synthesis, structure-activity relationship, and future prospects in drug development

Saleem Akbar , Subham Das , Rikeshwer Prasad Dewangan , Alex Joseph , Bahar Ahmed
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Abstract

1,3,4-Oxadiazine is a six-membered heterocyclic ring containing two nitrogen atoms and one oxygen atom. It is an important structural motif that has gained significant interest in the fields of pharmaceuticals, agrochemicals, and materials science due to its unique properties and versatile applications. The synthesis of 1,3,4-oxadiazine derivatives can be achieved through various methods such as cyclization of α,β-unsaturated nitriles, the reaction of hydrazides with carbonyl compounds, and condensation of nitriles with amidoximes. These synthetic routes offer a wide range of structural diversity and functionalization, making 1,3,4-oxadiazine derivatives attractive candidates for drug discovery and development. 1,3,4-Oxadiazine derivatives have been shown to possess a broad range of biological activities, including antitumor, antimicrobial, antiviral, and anti-inflammatory properties. During the literature search, it was observed that no review focuses on the SAR-based discussion of 1,3,4-oxadiazine ring-containing molecules used to treat various diseases. In order to address this issue in this review, we have discussed the synthetic route, US-granted patents, and structure-activity relationship (SAR) of the biologically active compound containing a 1,3,4-oxadiazine ring, as well as their current limitations and future prospects.

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综述 1,3,4-恶二嗪衍生物的潜力:合成、结构-活性关系以及药物开发的未来前景
1,3,4-恶二嗪是一种含有两个氮原子和一个氧原子的六元杂环。它是一种重要的结构基团,由于其独特的性质和广泛的应用,在制药、农用化学品和材料科学领域获得了极大的关注。1,3,4-噁二嗪衍生物的合成有多种方法,如 α,β-不饱和腈类的环化、酰肼与羰基化合物的反应以及腈类与脒氧肟的缩合。这些合成路线提供了广泛的结构多样性和功能化,使 1,3,4-恶二嗪衍生物成为药物发现和开发的诱人候选物质。1,3,4-恶二嗪衍生物已被证明具有广泛的生物活性,包括抗肿瘤、抗菌、抗病毒和抗炎特性。在文献检索过程中,我们发现没有一篇综述着重于对用于治疗各种疾病的含 1,3,4-恶二嗪环分子进行基于 SAR 的讨论。为了解决这个问题,我们在这篇综述中讨论了含有 1,3,4-恶二嗪环的生物活性化合物的合成路线、美国授予的专利和结构-活性关系(SAR),以及它们目前的局限性和未来的前景。
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