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Synthesis and evaluation of phenylisoserine derivatives for the SARS-CoV 3CL protease inhibitor.
Konno, Hiroyuki; Onuma, Takumi; Nitanai, Ikumi; Wakabayashi, Masaki; Yano, Shigekazu; Teruya, Kenta; Akaji, Kenichi.
Afiliação
  • Konno H; Department of Biological Engineering, Graduate School of Science and Engineering, Yamagata University, Yonezawa, Yamagata 992-8510, Japan. Electronic address: konno@yz.yamagata-u.ac.jp.
  • Onuma T; Department of Biological Engineering, Graduate School of Science and Engineering, Yamagata University, Yonezawa, Yamagata 992-8510, Japan.
  • Nitanai I; Department of Biological Engineering, Graduate School of Science and Engineering, Yamagata University, Yonezawa, Yamagata 992-8510, Japan.
  • Wakabayashi M; Department of Biological Engineering, Graduate School of Science and Engineering, Yamagata University, Yonezawa, Yamagata 992-8510, Japan.
  • Yano S; Department of Biological Engineering, Graduate School of Science and Engineering, Yamagata University, Yonezawa, Yamagata 992-8510, Japan.
  • Teruya K; Department of Neurochemistry, Tohoku University Graduate School of Medicine, Aoba-ku, Sendai 980-8575, Japan.
  • Akaji K; Department of Medicinal Chemistry, Kyoto Pharmaceutical University, Yamashina-ku, Kyoto 607-8414, Japan. Electronic address: akaji@mb.kyoto-phu.ac.jp.
Bioorg Med Chem Lett ; 27(12): 2746-2751, 2017 06 15.
Article em En | MEDLINE | ID: mdl-28454669
ABSTRACT
Synthesis and evaluation of new scaffold phenylisoserine derivatives connected with the essential functional groups against SARS CoV 3CL protease are described. The phenylisoserine backbone was found by simulation on GOLD software and the structure activity relationship study of phenylisoserine derivatives gave SK80 with an IC50 value of 43µM against SARS CoV 3CL R188I mutant protease.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Inibidores de Proteases / Serina / Proteínas Virais Limite: Humans Idioma: En Ano de publicação: 2017 Tipo de documento: Article
Texto completo
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PubMed Links
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Inibidores de Proteases / Serina / Proteínas Virais Limite: Humans Idioma: En Ano de publicação: 2017 Tipo de documento: Article