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Effect of prime-site sequence of retro-inverso-modified HTLV-1 protease inhibitor.
Awahara, Chiyuki; Tatsumi, Tadashi; Furuta, Saki; Shinjoh, Gen; Konno, Hiroyuki; Nosaka, Kazuto; Kobayashi, Kazuya; Hattori, Yasunao; Akaji, Kenichi.
Afiliação
  • Awahara C; Department of Chemistry, Graduate School of Medical Science, Kyoto Prefectural University of Medicine, Kita-ku, Kyoto 603-8334, Japan.
  • Tatsumi T; Department of Chemistry, Graduate School of Medical Science, Kyoto Prefectural University of Medicine, Kita-ku, Kyoto 603-8334, Japan.
  • Furuta S; Department of Medicinal Chemistry, Kyoto Pharmaceutical University, Yamashina-ku, Kyoto 607-8412, Japan.
  • Shinjoh G; Department of Medicinal Chemistry, Kyoto Pharmaceutical University, Yamashina-ku, Kyoto 607-8412, Japan.
  • Konno H; Department of Biochemical Engineering, Graduate School of Science and Technology, Yamagata University, Yonezawa, Yamagata 992-8510, Japan.
  • Nosaka K; Department of Chemistry, Hyogo College of Medicine, Nishinomiya, Hyogo 663-8501, Japan.
  • Kobayashi K; Department of Medicinal Chemistry, Kyoto Pharmaceutical University, Yamashina-ku, Kyoto 607-8412, Japan.
  • Hattori Y; Department of Medicinal Chemistry, Kyoto Pharmaceutical University, Yamashina-ku, Kyoto 607-8412, Japan.
  • Akaji K; Department of Medicinal Chemistry, Kyoto Pharmaceutical University, Yamashina-ku, Kyoto 607-8412, Japan. Electronic address: akaji@mb.kyoto-phu.ac.jp.
Bioorg Med Chem ; 22(8): 2482-8, 2014 Apr 15.
Article em En | MEDLINE | ID: mdl-24680060
ABSTRACT
The effects of additional substituents covering the prime-site of retro-inverso (RI)-modified HTLV-1 protease inhibitors containing a hydroxyethylamine isoster were clarified. Stereo-selective construction of the most potent isoster backbone was achieved by the Evans-aldol reaction. Addition of N-acetylated d-amino acid corresponding to the P2' site gave an RI-modified inhibitor showing superior inhibitory activity to the previous inhibitor. Inhibitory activities of the newly synthesized inhibitors suggest that partially modified RI inhibitors would interact with HTLV-1 protease in the same manner as the parent hydroxyethylamine inhibitor.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Inibidores de Proteases / Vírus Linfotrópico T Tipo 1 Humano / Ácido Aspártico Endopeptidases Limite: Humans Idioma: En Revista: Bioorg Med Chem Ano de publicação: 2014 Tipo de documento: Article
Texto completo
Imprimir
XML
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Inibidores de Proteases / Vírus Linfotrópico T Tipo 1 Humano / Ácido Aspártico Endopeptidases Limite: Humans Idioma: En Revista: Bioorg Med Chem Ano de publicação: 2014 Tipo de documento: Article