Selected article for: "activity compound and acute respiratory syndrome"

Author: Sup Shin, Young; Young Lee, Jun; Noh, Soojin; Kwak, Yoonna; Jeon, Sangeun; Kwon, Sunoh; Jin, Young-hee; Seong Jang, Min; Kim, Seungtaek; Hwan Song, Jong; Rae Kim, Hyoung; Min Park, Chul
Title: Discovery of Cyclic Sulfonamide derivatives as Potent Inhibitors of SARS-CoV-2
  • Cord-id: 1ee9aibw
  • Document date: 2020_11_4
  • ID: 1ee9aibw
    Snippet: 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 selectiv
    Document: 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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