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基于三嗪的抗癫痫药物的合成策略与构效关系研究:从实验室到临床的方法

Synthetic Strategies and SAR Studies of Triazine-Based Antiepileptic Agents: A Bench to Bedside Approach.

作者信息

Vats Nisha, Parveen Asiya, Shafeeque Mohd, Choudhary Akram, Yahya Shaikh, Yar M Shahar

机构信息

Department of Pharmaceutical Chemistry, School of Pharmaceutical Education and Research, Jamia Hamdard, New Delhi, India.

出版信息

Arch Pharm (Weinheim). 2025 May;358(5):e12004. doi: 10.1002/ardp.202500087.

DOI:10.1002/ardp.202500087
PMID:40345147
Abstract

Due to their strong biological activity, heterocyclic compounds containing triazine scaffolds are now of interest to a large number of organic chemists. It has been discovered that the triazine ring possesses antiepileptic properties. The article's goal is to highlight these particular ring diversities of study using triazine moieties that include medications and patent numbers. A variety of antiepileptic medications are being developed and will soon be available in the market to treat aberrant neuronal excitability. Among the key objectives to deal with a number of disorders affecting the central nervous system, such as epilepsy, chronic pain, mental illnesses, and spasticity, are voltage-gated sodium channel blockers. By blocking intricate voltage and frequency-dependent ionic currents via sodium channels, they prevent seizures. Although the sodium channel has been arguably the most extensively researched target for seizure control or treatment over the last 10 years, no ground-breaking findings have been made as of yet. Despite the fact that several medications are licensed to treat epilepsy, they are linked to a range of acute and long-term adverse effects. To treat epileptic seizures, multiple teams of researchers have been working nonstop to develop improved therapeutic medications for this well-liked target. The evolution of authorized sodium channel blockers as anticonvulsant medications is briefly noted in the study. To reduce the toxicity, medicinal chemists have attempted to create several stronger anticonvulsant medications, which are covered below. Their potential mechanism and structure-activity relationship (SAR) is highlighted.

摘要

由于其强大的生物活性,含三嗪骨架的杂环化合物目前受到众多有机化学家的关注。已发现三嗪环具有抗癫痫特性。本文的目的是突出使用包含药物和专利号的三嗪部分进行研究的这些特定环多样性。正在开发多种抗癫痫药物,不久将投放市场以治疗异常的神经元兴奋性。电压门控钠通道阻滞剂是应对影响中枢神经系统的多种疾病(如癫痫、慢性疼痛、精神疾病和痉挛)的关键目标之一。它们通过钠通道阻断复杂的电压和频率依赖性离子电流来预防癫痫发作。尽管在过去十年中,钠通道可以说是癫痫控制或治疗方面研究最广泛的靶点,但截至目前尚未有突破性发现。尽管有几种药物被批准用于治疗癫痫,但它们与一系列急性和长期不良反应有关。为了治疗癫痫发作,多个研究团队一直在不停地努力为这个热门靶点开发改进的治疗药物。该研究简要记录了已批准的钠通道阻滞剂作为抗惊厥药物的演变。为了降低毒性,药物化学家试图开发几种更强效的抗惊厥药物,如下所述。突出了它们的潜在机制和构效关系(SAR)。

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