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
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.
. 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
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.