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

ABSTRACT: 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 (IC50 = 0.88 ?M) against SARS-CoV-2 without cytotoxicity (CC50 > 25 ?M), 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.

SUBMITTER: Shin YS

PROVIDER: S-EPMC7640924 | biostudies-literature | 2020 Nov

REPOSITORIES: biostudies-literature

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

Shin Young Sup YS Lee Jun Young JY Noh Soojin S Kwak Yoonna Y Jeon Sangeun S Kwon Sunoh S Jin Young-Hee YH Jang Min Seong MS Kim Seungtaek S Song Jong Hwan JH Kim Hyoung Rae HR Park Chul Min CM

Bioorganic & medicinal chemistry letters 20201104

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 (IC50 = 0.88 μM) against SARS-CoV-2 without cytotoxicity (CC50 > 25 μM), ...[more]

PMID: 33160024

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