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Synthesis and biological evaluation of 3-acyl-2-phenylamino-1,4-dihydroquinolin-4(1H)-one derivatives as potential MERS-CoV inhibitors.
Yoon, Ji Hye; Lee, Jun Young; Lee, Jihye; Shin, Young Sup; Jeon, Sangeun; Kim, Dong Eon; Min, Jung Sun; Song, Jong Hwan; Kim, Seungtaek; Kwon, Sunoh; Jin, Young-Hee; Jang, Min Seong; Kim, Hyoung Rae; Park, Chul Min.
Afiliação
  • Yoon 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.
  • 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.
  • Lee J; Respiratory Virus Laboratory, Institut Pasteur Korea, Seongnam-si, Gyeonggi-do 13488, South Korea.
  • 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.
  • Jeon S; Respiratory Virus Laboratory, Institut Pasteur Korea, Seongnam-si, Gyeonggi-do 13488, South Korea.
  • Kim DE; Herbal Medicine Research Division, Korea Institute of Oriental Medicine, Daejeon 34054, South Korea.
  • Min JS; Herbal Medicine Research Division, Korea Institute of Oriental Medicine, Daejeon 34054, 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 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; Herbal Medicine Research Division, Korea Institute of Oriental Medicine, Daejeon 34054, South Korea.
  • Jang MS; Department of Non-Clinical Studies, Korea Institute of Toxicology, 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 ; 29(23): 126727, 2019 12 01.
Article em En | MEDLINE | ID: mdl-31624041
3-Acyl-2-phenylamino-1,4-dihydroquinolin-4(1H)-one derivatives were synthesized and evaluated to show high anti-MERS-CoV inhibitory activities. Among them, 6,8-difluoro-3-isobutyryl-2-((2,3,4-trifluorophenyl)amino)quinolin-4(1H)-one (6u) exhibits high inhibitory effect (IC50 = 86 nM) and low toxicity (CC50 > 25 µM). Moreover, it shows good metabolic stability, low hERG binding affinity, no cytotoxicity, and good in vivo PK properties.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Antivirais / Quinolonas / Coronavírus da Síndrome Respiratória do Oriente Médio Limite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2019 Tipo de documento: Article País de afiliação: Coréia do Sul
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Antivirais / Quinolonas / Coronavírus da Síndrome Respiratória do Oriente Médio Limite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2019 Tipo de documento: Article País de afiliação: Coréia do Sul