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Identification of 4-anilino-6-aminoquinazoline derivatives as potential MERS-CoV inhibitors.

Authors
  • Lee, Jun Young1
  • Shin, Young Sup1
  • Lee, Jihye2
  • Kwon, Sunoh3
  • Jin, Young-Hee4
  • Jang, Min Seong5
  • Kim, Seungtaek2
  • Song, Jong Hwan1
  • Kim, Hyoung Rae1
  • Park, Chul Min6
  • 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 Center for Convergent Research of Emerging Virus Infection (CEVI), Korea Research Institute of Chemical Technology, 141 Gajeong-ro, Yuseong-gu, Daejeon 34114, South Korea; Herbal Medicine Research Division, Korea Institute of Oriental Medicine, Daejeon 34054, South Korea. , (North Korea)
  • 4 Center for Convergent Research of Emerging Virus Infection (CEVI), Korea Research Institute of Chemical Technology, 141 Gajeong-ro, Yuseong-gu, Daejeon 34114, South Korea; KM Application Center, Korea Institute of Oriental Medicine, Dong-gu, Daegu 41062, South Korea. , (North Korea)
  • 5 Center for Convergent Research of Emerging Virus Infection (CEVI), Korea Research Institute of Chemical Technology, 141 Gajeong-ro, Yuseong-gu, Daejeon 34114, South Korea; Department of Non-Clinical Studies, Korea Institute of Toxicology, Yuseong-gu, Daejeon 34114, South Korea. , (North Korea)
  • 6 Center for Convergent Research of Emerging Virus Infection (CEVI), Korea Research Institute of Chemical Technology, 141 Gajeong-ro, Yuseong-gu, Daejeon 34114, South Korea. Electronic address: [email protected] , (North Korea)
Type
Published Article
Journal
Bioorganic & medicinal chemistry letters
Publication Date
Aug 08, 2020
Volume
30
Issue
20
Pages
127472–127472
Identifiers
DOI: 10.1016/j.bmcl.2020.127472
PMID: 32781216
Source
Medline
Keywords
Language
English
License
Unknown

Abstract

New therapies for treating coronaviruses are urgently needed. A series of 4-anilino-6-aminoquinazoline derivatives were synthesized and evaluated to show high anti-MERS-CoV activities. N4-(3-Chloro-4-fluorophenyl)-N6-(3-methoxybenzyl)quinazoline-4,6-diamine (1) has been identified in a random screen as a hit compound for inhibiting MERS-CoV infection. Throughout optimization process, compound 20 was found to exhibit high inhibitory effect (IC50 = 0.157 μM, SI = 25) with no cytotoxicity and moderate in vivo PK properties. Copyright © 2020 Elsevier Ltd. All rights reserved.

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