• Title of article

    Spirodiketopiperazine-based CCR5 antagonists: Lead optimization from biologically active metabolite

  • Author/Authors

    Rena Nishizawa، نويسنده , , Toshihiko Nishiyama، نويسنده , , Katsuya Hisaichi، نويسنده , , Naoki Matsunaga، نويسنده , , Chiaki Minamoto، نويسنده , , Hiromu Habashita، نويسنده , , Yoshikazu Takaoka، نويسنده , , Masaaki Toda، نويسنده , , Shiro Shibayama، نويسنده , , Hideaki Tada، نويسنده , , Kenji Sagawa، نويسنده , , Daikichi Fukushima، نويسنده , , Kenji Maeda، نويسنده , , Hiroaki Mitsuya، نويسنده ,

  • Issue Information
    روزنامه با شماره پیاپی سال 2007
  • Pages
    5
  • From page
    727
  • To page
    731
  • Abstract
    Hydroxylated derivatives were designed and synthesized based on the information of oxidative metabolites. Compounds derived from β-substituted (2R,3R)-2-amino-3-hydroxypropionic acid showed improved inhibitory activities against the binding of MIP-1α to human CCR5, compared with the non-hydroxylated derivatives and the other isomers.
  • Keywords
    CCR5 , HIV-1 , Active metabolite
  • Journal title
    Bioorganic & Medicinal Chemistry Letters
  • Serial Year
    2007
  • Journal title
    Bioorganic & Medicinal Chemistry Letters
  • Record number

    797728