tetano
Editor, Senior Moderator
Bioorg Med Chem Lett
. 2020 Nov 4;127667.
doi: 10.1016/j.bmcl.2020.127667. Online ahead of print.
Discovery of Cyclic Sulfonamide derivatives as Potent Inhibitors of SARS-CoV-2
Young Sup Shin[SUP] 1 [/SUP], Jun Young Lee[SUP] 1 [/SUP], Soojin Noh[SUP] 1 [/SUP], Yoonna Kwak[SUP] 1 [/SUP], Sangeun Jeon[SUP] 2 [/SUP], Sunoh Kwon[SUP] 3 [/SUP], Young-Hee Jin[SUP] 4 [/SUP], Min Seong Jang[SUP] 5 [/SUP], Seungtaek Kim[SUP] 2 [/SUP], Jong Hwan Song[SUP] 1 [/SUP], Hyoung Rae Kim[SUP] 1 [/SUP], Chul Min Park[SUP] 1 [/SUP]
Affiliations
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 (IC[SUB]50[/SUB] = 0.88 μM) against SARS-CoV-2 without cytotoxicity (CC[SUB]50[/SUB] > 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.
. 2020 Nov 4;127667.
doi: 10.1016/j.bmcl.2020.127667. Online ahead of print.
Discovery of Cyclic Sulfonamide derivatives as Potent Inhibitors of SARS-CoV-2
Young Sup Shin[SUP] 1 [/SUP], Jun Young Lee[SUP] 1 [/SUP], Soojin Noh[SUP] 1 [/SUP], Yoonna Kwak[SUP] 1 [/SUP], Sangeun Jeon[SUP] 2 [/SUP], Sunoh Kwon[SUP] 3 [/SUP], Young-Hee Jin[SUP] 4 [/SUP], Min Seong Jang[SUP] 5 [/SUP], Seungtaek Kim[SUP] 2 [/SUP], Jong Hwan Song[SUP] 1 [/SUP], Hyoung Rae Kim[SUP] 1 [/SUP], Chul Min Park[SUP] 1 [/SUP]
Affiliations
- PMID: 33160024
- DOI: 10.1016/j.bmcl.2020.127667
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 (IC[SUB]50[/SUB] = 0.88 μM) against SARS-CoV-2 without cytotoxicity (CC[SUB]50[/SUB] > 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.