1,2,4-苯并噻二嗪-1,1-二氧化物的生物活性研究进展  

Research progress on biological activity of 1,2,4-benzothiadiazine-1,1-dioxide

作　　者：何兆龙 邹瑜 陈霞[1] 赵文豪 胡雯[1] 徐诗强[1] HE Zhaolong;ZOU Yu;CHEN Xia;ZHAO Wenhao;HU Wen;XU Shiqiang(Wuhan University of Science and Technology,Wuhan 430065,China)

机构地区：[1]武汉科技大学,湖北武汉430065

出　　处：《药学研究》2025年第1期56-65,共10页Journal of Pharmaceutical Research

基　　金：国家自然科学基金项目(No.82003593)。

摘　　要：1,2,4-苯并噻二嗪-1,1-二氧化物的代表性药物氯噻嗪被广泛应用于临床治疗,具有利尿和降压作用。近年来,以1,2,4-苯并噻二嗪-1,1-二氧化物为母核的化合物展现出改善认知功能、抗肿瘤、抗菌和抗病毒等多种药理活性,因此该类化合物已成为当前研究的热点。本文系统总结了近年来1,2,4-苯并噻二嗪-1,1-二氧化物衍生物的国内外研究成果,重点综述了其结构改造和活性研究进展,总结发现1,2,4-苯并噻二嗪-1,1-二氧化物可以作为α-氨基-3-羟基-5-甲基-4-异恶唑丙酸(AMPA)和红藻氨酸(KA)受体变构调节剂改善神经功能;对PI3K等癌症相关靶点具有较好的抑制活性;通过抑制HCV NS5B聚合酶发挥抗病毒活性;对糖尿病相关疾病靶点如醛糖还原酶、丙酮酸脱氢酶具有较高抑制活性;此外,该类化合物在抗菌、抗虫和抗氧化等方面也有新的研究进展。本文汇总了这些研究成果并分析了其构效关系,旨在为广大研究人员提供研究依据和思路。The representative drug of 1,2,4-benzothiadiazine-1,1-dioxide chlorthiazide is widely used in clinical treatment and has diuretic and antihypertensive effects.In recent years,compounds with 1,2,4-benzothiadiazine-1,1-dioxide as the parent nucleus have shown various pharmacological activities such as improvement of cognitive function,anti-tumour,antibacterial and antiviral activities,so this class of compounds has become a hot topic of current research.In this paper,the research achievements of 1,2,4-benzothiadiazine-1,1-dioxide derivatives at home and abroad in recent years were systematically reviewed,with emphasis on the progress of structural modification and activity research.It was concluded that 1,2,4-benzothiadiazine-1,1-dioxide can be used as positive allosteric modulators(PAMs)of AMPA and KA receptors to improve nerve function;It has good inhibitory activity against cancer-related targets such as PI3K;It can inhibit HCV NS5B polymerase to exert antiviral activity;And it has high inhibition activity against diabetes-related disease targets such as aldose reductase and pyruvate dehydrogenase;In addition,the compounds have made new progress in antibacterial,anti-insect and anti-oxidation,this paper summarized these research results and analyzed the structure-activity relationship to provide research basis and ideas for the majority of researchers.

关 键 词：1 2 4-苯并噻二嗪-1 1-二氧化物 研究进展 中枢神经兴奋作用 抗肿瘤 抗病毒 糖尿病 

分 类 号：R961[医药卫生—药理学]