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10.1016/j.bmcl.2020.127667

http://scihub22266oqcxt.onion/10.1016/j.bmcl.2020.127667
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33160024!7640924!33160024
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suck abstract from ncbi

pmid33160024      Bioorg+Med+Chem+Lett 2021 ; 31 (?): 127667
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  • Discovery of cyclic sulfonamide derivatives as potent inhibitors of SARS-CoV-2 #MMPMID33160024
  • Shin YS; Lee JY; Noh S; Kwak Y; Jeon S; Kwon S; Jin YH; Jang MS; Kim S; Song JH; Kim HR; Park CM
  • Bioorg Med Chem Lett 2021[Jan]; 31 (?): 127667 PMID33160024show ga
  • 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 muM) against SARS-CoV-2 without cytotoxicity (CC(50) > 25 muM), 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.
  • |*Drug Discovery[MESH]
  • |Animals[MESH]
  • |Antiviral Agents/chemical synthesis/chemistry/*pharmacology[MESH]
  • |COVID-19 Drug Treatment[MESH]
  • |Cell Line[MESH]
  • |Chlorocebus aethiops[MESH]
  • |Cricetulus[MESH]
  • |Dogs[MESH]
  • |Dose-Response Relationship, Drug[MESH]
  • |Humans[MESH]
  • |Mice[MESH]
  • |Microbial Sensitivity Tests[MESH]
  • |Molecular Structure[MESH]
  • |Rats[MESH]
  • |SARS-CoV-2/*drug effects[MESH]
  • |Structure-Activity Relationship[MESH]


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