抗疟药的研究——Ⅲ.2-(取代苯乙烯基)-4-氨基吡啶类的合成

本文报道2-(取代苯乙烯基)-4-(4′-二乙氨基-1′-甲基丁基氨基)-吡啶类的合成。动物筛选的初步结果表明:口服给药6.25mg/kg,化合物Ⅲ₂、Ⅲ₄和Ⅲ₇能完全抑制感染伯氏鼠疟原虫氯喹敏感株(Plalmodium berghei)小白鼠的原虫血症;皮下给药1.8mg/kg,化合物Ⅲ,即能达到完全抑制。

Studies on antimalarials. III. Synthesis of 2-(substituted styryl)-4-amino pyridines

Nine 2-(substituted styryl)-4-amino, pyridines Ⅲ and three 2-(substituted styryl)-6-methyl-4-amino pyridines IV have been synthesized by condensation of 4-(4'-diethyl amino-1'-methyl amino)-2-methyl (or 2,6-dimethyl)-pyridine-with substituted aryl aldehydes.Preliminary results showed that compounds Ⅲ₂, Ⅲ₄ and Ⅲ₇ exhibited notable antimalarial activity against chloroquine-sensitive strain of P. berghei in mice at 6.25mg/kg after oral administration. Compound Ⅲ₇ can suppress parasitemia of mice infected with chloroquine-sensitive strain of P. berghei at 1.8 mg/kg subcutaneously. Among them Ⅲ₇ was the most active.