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

Authors
  • Shin, Young Sup1
  • Lee, Jun Young1
  • Noh, Soojin1
  • Kwak, Yoonna1
  • Jeon, Sangeun2
  • Kwon, Sunoh3
  • Jin, Young-Hee4
  • Jang, Min Seong5
  • Kim, Seungtaek2
  • Song, Jong Hwan1
  • Kim, Hyoung Rae1
  • Park, Chul Min1
  • 1 Center for Convergent Research of Emerging Virus Infection (CEVI), Korea Research Institute of Chemical Technology, 141 Gajeong-ro, Yuseong-gu, Daejeon 34114, South Korea. , (North Korea)
  • 2 Zoonotic Virus Laboratory, Institut Pasteur Korea, Seongnam-si, Gyeonggi-do 13488, South Korea. , (North Korea)
  • 3 Herbal Medicine Research Division, Korea Institute of Oriental Medicine, Daejeon 34054, South Korea. , (North Korea)
  • 4 KM Application Center, Korea Institute of Oriental Medicine, Dong-gu, Daegu 41062, South Korea. , (North Korea)
  • 5 Department of Non-Clinical Studies, Korea Institute of Toxicology, Yuseong-gu, Daejeon 34114, South Korea. , (North Korea)
Type
Published Article
Journal
Bioorganic & medicinal chemistry letters
Publication Date
Jan 01, 2021
Volume
31
Pages
127667–127667
Identifiers
DOI: 10.1016/j.bmcl.2020.127667
PMID: 33160024
Source
Medline
Keywords
Language
English
License
Unknown

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. Copyright © 2020 Elsevier Ltd. All rights reserved.

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