Research progress on biological activity of 1,2,4-benzothiadiazine-1,1-dioxide
HE Zhaolong
ZOU Yu
CHEN Xia
ZHAO Wenhao
HU Wen
XU Shiqiang
Abstract：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-diox-ide 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.
Keywords：124-benzothiadiazine-11-dioxideResearch progressCentral nervous excitatory offectAnti-tumorAntiviralDiabetes
Publication Date：2025-01-27
Online Publishing Date：2025-08-15(First online date of this platform, not the publication date of the document)
Pages：10( 56-65 )