{"title":"新型磺胺衍生物作为Nav1.5钠通道阻滞剂治疗心房颤动","authors":"Siyan Feng, and , Steven H. Liang*, ","doi":"10.1021/acsmedchemlett.5c0019210.1021/acsmedchemlett.5c00192","DOIUrl":null,"url":null,"abstract":"<p >This highlight describes a novel class of sulfonamide-based Nav1.5 sodium channel blockers. These compounds preferentially inhibit Nav1.5 in atrial cardiomyocytes, extending the effective refractory period and preventing arrhythmic, rapid contraction of the atria. The novel Nav1.5 blockers possess the potential to treat Atrial Fibrillation without affecting the function of the rest of the heart.</p>","PeriodicalId":20,"journal":{"name":"ACS Medicinal Chemistry Letters","volume":"16 5","pages":"748–749 748–749"},"PeriodicalIF":3.5000,"publicationDate":"2025-04-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Novel Sulfonamide Derivatives as Nav1.5 Sodium Channel Blockers for Treating Atrial Fibrillation\",\"authors\":\"Siyan Feng, and , Steven H. Liang*, \",\"doi\":\"10.1021/acsmedchemlett.5c0019210.1021/acsmedchemlett.5c00192\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p >This highlight describes a novel class of sulfonamide-based Nav1.5 sodium channel blockers. These compounds preferentially inhibit Nav1.5 in atrial cardiomyocytes, extending the effective refractory period and preventing arrhythmic, rapid contraction of the atria. The novel Nav1.5 blockers possess the potential to treat Atrial Fibrillation without affecting the function of the rest of the heart.</p>\",\"PeriodicalId\":20,\"journal\":{\"name\":\"ACS Medicinal Chemistry Letters\",\"volume\":\"16 5\",\"pages\":\"748–749 748–749\"},\"PeriodicalIF\":3.5000,\"publicationDate\":\"2025-04-21\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"ACS Medicinal Chemistry Letters\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://pubs.acs.org/doi/10.1021/acsmedchemlett.5c00192\",\"RegionNum\":3,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q2\",\"JCRName\":\"CHEMISTRY, MEDICINAL\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"ACS Medicinal Chemistry Letters","FirstCategoryId":"3","ListUrlMain":"https://pubs.acs.org/doi/10.1021/acsmedchemlett.5c00192","RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}
Novel Sulfonamide Derivatives as Nav1.5 Sodium Channel Blockers for Treating Atrial Fibrillation
This highlight describes a novel class of sulfonamide-based Nav1.5 sodium channel blockers. These compounds preferentially inhibit Nav1.5 in atrial cardiomyocytes, extending the effective refractory period and preventing arrhythmic, rapid contraction of the atria. The novel Nav1.5 blockers possess the potential to treat Atrial Fibrillation without affecting the function of the rest of the heart.
期刊介绍:
ACS Medicinal Chemistry Letters is interested in receiving manuscripts that discuss various aspects of medicinal chemistry. The journal will publish studies that pertain to a broad range of subject matter, including compound design and optimization, biological evaluation, drug delivery, imaging agents, and pharmacology of both small and large bioactive molecules. Specific areas include but are not limited to:
Identification, synthesis, and optimization of lead biologically active molecules and drugs (small molecules and biologics)
Biological characterization of new molecular entities in the context of drug discovery
Computational, cheminformatics, and structural studies for the identification or SAR analysis of bioactive molecules, ligands and their targets, etc.
Novel and improved methodologies, including radiation biochemistry, with broad application to medicinal chemistry
Discovery technologies for biologically active molecules from both synthetic and natural (plant and other) sources
Pharmacokinetic/pharmacodynamic studies that address mechanisms underlying drug disposition and response
Pharmacogenetic and pharmacogenomic studies used to enhance drug design and the translation of medicinal chemistry into the clinic
Mechanistic drug metabolism and regulation of metabolic enzyme gene expression
Chemistry patents relevant to the medicinal chemistry field.