122(P68) 免疫抑制活性物質ISP-I (Myriocin)の活性発現に必要な最小基礎構造(2-Aminoalcohol)の探索(ポスター発表の部)

概要

論文の詳細を見る
2-Aminoalcohol was shown to be the minimum essential structure for the immunosuppressive activity of 2-alkyl-2-aminopropane-1,3-diol, which was generated by modification of ISP-I (1: myriocin, thermozymocidin). 2-Aminoalcohols 4a-h were examined for immunosuppressive activity on mouse allogeneic mixed lymphocyte reaction (MLR) in vitro. The series showed a bell-shaped relationship between the activity and the carbon numbers. Among them, 2-aminohexadecanol (4c) was the most potent. In order to investigate relationship between the activity and the configuration at C-2 in 2-aminoalcohol, (R)- and (S)-isomers of 4c, 2-aminoeicosanol (4h) and 2-amino-4-(4-octylphenyl)butanol (5) were prepared and examined for the activity on mouse allogeneic MLR. As a results, the (R)-isomers were more potent the (S)-isomers, and (R)-4c displayed comparably activity to FTY720 (3), which is expected as a powerful candidate for safer immunosuppressant for organ transplantations and for the treatment of autoimmune diseases.
天然有機化合物討論会の論文
1996-09-02