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Bioorg Med Chem Lett . Synthesis and evaluation of N-arylindazole-3-carboxamide derivatives as novel antiviral agents against SARS-CoV-2

tetano

tetano

Editor, Senior Moderator
Bioorg Med Chem Lett


. 2024 Nov 1:130015.
doi: 10.1016/j.bmcl.2024.130015. Online ahead of print. Synthesis and evaluation of N-arylindazole-3-carboxamide derivatives as novel antiviral agents against SARS-CoV-2

Jun Young Lee[SUP] 1 [/SUP], Sangeun Jeon[SUP] 2 [/SUP], Jung-Eun Cho[SUP] 3 [/SUP], Sungmin Kim[SUP] 3 [/SUP], Hyoung Rae Kim[SUP] 3 [/SUP], Hyeung-Geun Park[SUP] 4 [/SUP], Seungtaek Kim[SUP] 5 [/SUP], Chul Min Park[SUP] 6 [/SUP]



Affiliations
Abstract

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 (EC[SUB]50[/SUB] = 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.

Keywords: Antiviral; Coronavirus; MERS-CoV; N-Arylindazole-3-carboxamide; SARS-CoV-2.

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