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合成2,4-二氨基-6-(N-取代-对氯苄氨基)喹唑啉衍生物33个,经伯氏鼠疟原虫(Plasmodium berghei)抑制性治疗筛选,剂量20mg/kg×3d,有10个化合物(1,2,5～8,14,20,21,26)抑制率在90％以上。经约氏鼠疟原虫(P.yoelii)斯氏按蚊系统的病因性预防筛选,剂量5mg/kg×3d,有26个化合物(1～12,14,20～22,24～33)使小白鼠全部得到保护;剂量下降到0.625mg/kg×3d,有14个化合物(5～12,14,20,21,26,31,33)使小白鼠全部得到保护(表1)。4个化合物(1,8,20,25,表2,3)进行了猴疟(P.cynomolgi)试验,效果不及伯喹和乙胺嘧啶。
Thirty-three 2,4-diamino-6- (N-substituted-p-chlorobenzylamino) quinazoline derivatives were synthesized and used for the screening of inhibitory treatment with Plasmodium berghei at a dose of 20 mg / kg × 3d, 10 compounds (1,2,5 ~ 8,14,20,21,26) inhibition rate of 90% or more. The etiology of P. yoelii An. Mosquito system was screened at a dose of 5 mg / kg × 3d, with 26 compounds (1 ~ 12,14,20 ~ 22,24 ~ 33) All mice were protected; the dose was reduced to 0.625mg / kg × 3d, and 14 compounds (5 ~ 12,14,20,21,26,31,33) were all protected mice (Table 1). Four compounds (1, 8, 20, 25, Tables 2 and 3) were tested for P. cygnomoli less well than either primaquine or pyrimethamine.