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

[tetano]

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 ¹ , Sangeun Jeon ² , Jung-Eun Cho ³ , Sungmin Kim ³ , Hyoung Rae Kim ³ , Hyeung-Geun Park ⁴ , Seungtaek Kim ⁵ , Chul Min Park ⁶



Affiliations

• PMID: 39489229
• DOI: 10.1016/j.bmcl.2024.130015

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 (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.

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