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

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。

Synthesis and evaluation of N-arylindazole-3-carboxamide derivatives as novel antiviral agents against SARS-CoV-2

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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.

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来源期刊

Bioorganic & Medicinal Chemistry Letters 医学-医药化学

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.