本文报道了2,4-二氨基-6-N~1,N~2-二取代肼基-喹唑啉类衍生物的合成及其抗疟活性的研究。这类化合物的合成是以2,4-二氨基6-取代苄基氨基-喹唑啉为原料经亚硝化、还原成为2,4-二氨基6-(N~1-取代苄基)—肼基喹唑啉,再与相应的醛缩合而成。此类化合物经伯氏鼠疟原虫抑制性治疗初筛表明有少数具有一定的效果。有11个化合物经约氏鼠疟原虫—斯氏按蚊系统病因性初筛有效。其中化合物Ⅱ_(1,7,8,11,16)和Ⅲ_1口服2.5mg/kg,连续3天,可使受试小鼠全部得到保护。 In this paper, the synthesis of 2,4-diamino-6-N ~ 1, N ~ 2-substituted hydrazino-quinazoline derivatives and their anti-malarial activity were reported. The synthesis of these compounds is based on the 2,4-diamino-6-substituted benzylamino-quinazoline as the raw material by nitrosation, reduced to 2,4-diamino 6- (N ~ 1-substituted benzyl) - hydrazine Quinazoline, and then with the corresponding aldehyde condensation. The first screening of these compounds by inhibition of P. berberis showed that a few had some effect. Eleven compounds were validated by etiological screening of P.japonicus-An. Compounds Ⅱ_ (1,7,8,11,16) and Ⅲ_1 oral 2.5mg / kg, for 3 days, all mice can be protected.