合成和评估 N-芳基吲唑-3-甲酰胺衍生物作为抗 SARS-CoV-2 的新型抗病毒药物。

IF 2.5 4区 医学 Q3 CHEMISTRY, MEDICINAL Bioorganic & Medicinal Chemistry Letters Pub Date : 2024-11-01 DOI:10.1016/j.bmcl.2024.130015
Jun Young Lee , Sangeun Jeon , Jung-Eun Cho , Sungmin Kim , Hyoung Rae Kim , Hyeung-geun Park , Seungtaek Kim , Chul Min Park
{"title":"合成和评估 N-芳基吲唑-3-甲酰胺衍生物作为抗 SARS-CoV-2 的新型抗病毒药物。","authors":"Jun Young Lee ,&nbsp;Sangeun Jeon ,&nbsp;Jung-Eun Cho ,&nbsp;Sungmin Kim ,&nbsp;Hyoung Rae Kim ,&nbsp;Hyeung-geun Park ,&nbsp;Seungtaek Kim ,&nbsp;Chul Min Park","doi":"10.1016/j.bmcl.2024.130015","DOIUrl":null,"url":null,"abstract":"<div><div><em>N</em>-Arylindazole-3-carboxamide derivatives synthesized from an anti-MERS-CoV hit compound showed potent inhibitory activities against SARS-CoV-2. Among them, 5-chloro-<em>N</em>-(3,5-dichlorophenyl)-1<em>H</em>-indazole-3-carboxamide (<strong>4a</strong>) exhibited a potent inhibitory effect (EC<sub>50</sub> = 0.69 µM), low cytotoxicity, and satisfactory <em>in vitro</em> PK profiles. Thus, <em>N</em>-arylindazole-3-carboxamide <strong>4a</strong> provides a novel template for future development of anti-coronavirus agents.</div></div>","PeriodicalId":256,"journal":{"name":"Bioorganic & Medicinal Chemistry Letters","volume":null,"pages":null},"PeriodicalIF":2.5000,"publicationDate":"2024-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Synthesis and evaluation of N-arylindazole-3-carboxamide derivatives as novel antiviral agents against SARS-CoV-2\",\"authors\":\"Jun Young Lee ,&nbsp;Sangeun Jeon ,&nbsp;Jung-Eun Cho ,&nbsp;Sungmin Kim ,&nbsp;Hyoung Rae Kim ,&nbsp;Hyeung-geun Park ,&nbsp;Seungtaek Kim ,&nbsp;Chul Min Park\",\"doi\":\"10.1016/j.bmcl.2024.130015\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><div><em>N</em>-Arylindazole-3-carboxamide derivatives synthesized from an anti-MERS-CoV hit compound showed potent inhibitory activities against SARS-CoV-2. Among them, 5-chloro-<em>N</em>-(3,5-dichlorophenyl)-1<em>H</em>-indazole-3-carboxamide (<strong>4a</strong>) exhibited a potent inhibitory effect (EC<sub>50</sub> = 0.69 µM), low cytotoxicity, and satisfactory <em>in vitro</em> PK profiles. Thus, <em>N</em>-arylindazole-3-carboxamide <strong>4a</strong> provides a novel template for future development of anti-coronavirus agents.</div></div>\",\"PeriodicalId\":256,\"journal\":{\"name\":\"Bioorganic & Medicinal Chemistry Letters\",\"volume\":null,\"pages\":null},\"PeriodicalIF\":2.5000,\"publicationDate\":\"2024-11-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Bioorganic & Medicinal Chemistry Letters\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/S0960894X24004177\",\"RegionNum\":4,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q3\",\"JCRName\":\"CHEMISTRY, MEDICINAL\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Bioorganic & Medicinal Chemistry Letters","FirstCategoryId":"3","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S0960894X24004177","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}
引用次数: 0

摘要

由一种抗MERS-CoV命中化合物合成的N-芳基吲唑-3-甲酰胺衍生物对SARS-CoV-2有很强的抑制作用。其中,5-氯-N-(3,5-二氯苯基)-1H-吲唑-3-甲酰胺(4a)具有强效抑制作用(EC50 = 0.69 µM)、低细胞毒性和令人满意的体外 PK 曲线。因此,N-芳基吲唑-3-甲酰胺 4a 为今后开发抗冠状病毒药物提供了新的模板。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

摘要图片

查看原文
分享 分享
微信好友 朋友圈 QQ好友 复制链接
本刊更多论文
Synthesis and evaluation of N-arylindazole-3-carboxamide derivatives as novel antiviral agents against SARS-CoV-2
N-Arylindazole-3-carboxamide derivatives synthesized from an anti-MERS-CoV hit compound showed potent inhibitory activities against SARS-CoV-2. Among them, 5-chloro-N-(3,5-dichlorophenyl)-1H-indazole-3-carboxamide (4a) exhibited a potent inhibitory effect (EC50 = 0.69 µM), low cytotoxicity, and satisfactory in vitro PK profiles. Thus, N-arylindazole-3-carboxamide 4a provides a novel template for future development of anti-coronavirus agents.
求助全文
通过发布文献求助,成功后即可免费获取论文全文。 去求助
来源期刊
CiteScore
5.70
自引率
3.70%
发文量
463
审稿时长
27 days
期刊介绍: Bioorganic & Medicinal Chemistry Letters presents preliminary experimental or theoretical research results of outstanding significance and timeliness on all aspects of science at the interface of chemistry and biology and on major advances in drug design and development. The journal publishes articles in the form of communications reporting experimental or theoretical results of special interest, and strives to provide maximum dissemination to a large, international audience.
期刊最新文献
Structural basis of the C-terminal domain of SARS-CoV-2 N protein in complex with GMP reveals critical residues for RNA interaction Synthesis and evaluation of N-arylindazole-3-carboxamide derivatives as novel antiviral agents against SARS-CoV-2 Synthesis, highly potent α-glucosidase inhibition, antioxidant and molecular docking of various novel dihydropyrimidine derivatives to treat diabetes mellitus. A convenient approach for generating dimeric nucleic acid dyes via click-chemistry Computational approach based on freely accessible tools for antimicrobial drug design.
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
×
提示
您的信息不完整,为了账户安全,请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
现在去查看 取消
×
提示
确定
0
微信
客服QQ
Book学术公众号 扫码关注我们
反馈
×
意见反馈
请填写您的意见或建议
请填写您的手机或邮箱
已复制链接
已复制链接
快去分享给好友吧!
我知道了
×
扫码分享
扫码分享
Book学术官方微信
Book学术文献互助
Book学术文献互助群
群 号:481959085
Book学术
文献互助 智能选刊 最新文献 互助须知 联系我们:info@booksci.cn
Book学术提供免费学术资源搜索服务,方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。
Copyright © 2023 Book学术 All rights reserved.
ghs 京公网安备 11010802042870号 京ICP备2023020795号-1