新型CD4抑制剂J2的合成及其活性评价

Synthesis of J2 as a novel CD4 antagonist

以1-氯-2,4-二硝基苯为原料,经与甲胺反应,再氢化还原,在DCC存在条件下与3-吲哚丙烯酸缩合得到CD4抑制剂J2,总收率39.4%;通过混合淋巴细胞试验、细胞黏附试验和小鼠肾移植试验评价其免疫抑制活性,结果显示J2能够阻断MHC-Ⅱ与CD4分子的结合,是一个具有较强活性的免疫抑制剂。

1-Chloro-2,4-dinitro-benzene was used as the original material, after reaction with methylamine, then hydrogenation and reaction with（E）-3-（1H-indol-3-yl） -acrylic acid in the present of DCC to synthesize J2 ,the total yield of this method is 39.4%. Its bioactivities were evaluated by mixed leukocyte reaction assays,cell adhesion assays and murine kidney allograft rejection assays. And it was found that J2 could block the interaction between CD4 and MHC- Ⅱ, to be a potent immunosuppressive agent.