Discovery of cyclic sulfonamide derivatives as potent inhibitors of SARS-CoV-2

Severe Acute Respiratory Syndrome Coronavirus-2 (SARS-CoV-2) continues to spread worldwide, with 25 million confirmed cases and 800 thousand deaths. Effective treatments to target SARS-CoV-2 are urgently needed. In the present study, we have identified a class of cyclic sulfonamide derivatives as no...

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Detalles Bibliográficos
Autores principales: Shin, Young Sup, Lee, Jun Young, Noh, Soojin, Kwak, Yoonna, Jeon, Sangeun, Kwon, Sunoh, Jin, Young-hee, Jang, Min Seong, Kim, Seungtaek, Song, Jong Hwan, Kim, Hyoung Rae, Park, Chul Min
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Elsevier Ltd. 2021
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7640924/
https://www.ncbi.nlm.nih.gov/pubmed/33160024
http://dx.doi.org/10.1016/j.bmcl.2020.127667
Descripción
Sumario:Severe Acute Respiratory Syndrome Coronavirus-2 (SARS-CoV-2) continues to spread worldwide, with 25 million confirmed cases and 800 thousand deaths. Effective treatments to target SARS-CoV-2 are urgently needed. In the present study, we have identified a class of cyclic sulfonamide derivatives as novel SARS-CoV-2 inhibitors. Compound 13c of the synthesized compounds exhibited robust inhibitory activity (IC(50) = 0.88 μM) against SARS-CoV-2 without cytotoxicity (CC(50) > 25 μM), with a selectivity index (SI) of 30.7. In addition, compound 13c exhibited high oral bioavailability (77%) and metabolic stability with good safety profiles in hERG and cytotoxicity studies. The present study identified that cyclic sulfonamide derivatives are a promising new template for the development of anti-SARS-CoV-2 agents.

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