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Discovery of cyclic sulfonamide derivatives as potent inhibitors of SARS-CoV-2.
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.
  • Shin YS; Center for Convergent Research of Emerging Virus Infection (CEVI), Korea Research Institute of Chemical Technology, 141 Gajeong-ro, Yuseong-gu, Daejeon 34114, South Korea.
  • Lee JY; Center for Convergent Research of Emerging Virus Infection (CEVI), Korea Research Institute of Chemical Technology, 141 Gajeong-ro, Yuseong-gu, Daejeon 34114, South Korea.
  • Noh S; Center for Convergent Research of Emerging Virus Infection (CEVI), Korea Research Institute of Chemical Technology, 141 Gajeong-ro, Yuseong-gu, Daejeon 34114, South Korea.
  • Kwak Y; Center for Convergent Research of Emerging Virus Infection (CEVI), Korea Research Institute of Chemical Technology, 141 Gajeong-ro, Yuseong-gu, Daejeon 34114, South Korea.
  • Jeon S; Zoonotic Virus Laboratory, Institut Pasteur Korea, Seongnam-si, Gyeonggi-do 13488, South Korea.
  • Kwon S; Herbal Medicine Research Division, Korea Institute of Oriental Medicine, Daejeon 34054, South Korea.
  • Jin YH; KM Application Center, Korea Institute of Oriental Medicine, Dong-gu, Daegu 41062, South Korea.
  • Jang MS; Department of Non-Clinical Studies, Korea Institute of Toxicology, Yuseong-gu, Daejeon 34114, South Korea.
  • Kim S; Zoonotic Virus Laboratory, Institut Pasteur Korea, Seongnam-si, Gyeonggi-do 13488, South Korea.
  • Song JH; Center for Convergent Research of Emerging Virus Infection (CEVI), Korea Research Institute of Chemical Technology, 141 Gajeong-ro, Yuseong-gu, Daejeon 34114, South Korea.
  • Kim HR; Center for Convergent Research of Emerging Virus Infection (CEVI), Korea Research Institute of Chemical Technology, 141 Gajeong-ro, Yuseong-gu, Daejeon 34114, South Korea.
  • Park CM; Center for Convergent Research of Emerging Virus Infection (CEVI), Korea Research Institute of Chemical Technology, 141 Gajeong-ro, Yuseong-gu, Daejeon 34114, South Korea.
Bioorg Med Chem Lett ; 31: 127667, 2021 01 01.
Article in English | MEDLINE | ID: covidwho-907172
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 µM) against SARS-CoV-2 without cytotoxicity (CC50 > 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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Full text: Available Collection: International databases Database: MEDLINE Main subject: Antiviral Agents / Sulfonamides / Drug Discovery / SARS-CoV-2 Limits: Animals / Humans Language: English Journal: Bioorg Med Chem Lett Journal subject: Biochemistry / Chemistry Year: 2021 Document Type: Article Affiliation country: J.bmcl.2020.127667

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Full text: Available Collection: International databases Database: MEDLINE Main subject: Antiviral Agents / Sulfonamides / Drug Discovery / SARS-CoV-2 Limits: Animals / Humans Language: English Journal: Bioorg Med Chem Lett Journal subject: Biochemistry / Chemistry Year: 2021 Document Type: Article Affiliation country: J.bmcl.2020.127667