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本文报道2,4-二氨基-5-取代氨基嘧啶和2,4-二氨基-6-甲基-5-取代氨基嘧啶衍生物的合成及其抗疟活性的研究。这类化合物的合成是分别以2,4,5-三氨基嘧啶或2,4,5-三氨基-6-甲基嘧啶与相应的取代的苯甲醛缩合成席夫氏碱,然后经还原,亚硝化或甲酰化制得。经鼠疟原虫-斯氏按蚊系统的病因性预防初筛,发现有12个化合物有效,其中2,4-二氨基5-[(3′,4′-二氯代苯亚甲基)-氨基]嘧啶(化合物V_3)和2,4-二氨基-5-[(4′-溴代苄基)-N-亚硝基-氨基]嘧啶(化合物Ⅶ_4)效果最好,口服10 mg/kg共三天,可使小白鼠得到保护,血中未查见原虫。
This paper reports the synthesis of 2,4-diamino-5-substituted aminopyrimidines and 2,4-diamino-6-methyl-5-substituted aminopyrimidines and their antimalarial activity. The synthesis of these compounds is the condensation of 2,4,5-triaminopyrimidine or 2,4,5-triamino-6-methylpyrimidine with the corresponding substituted benzaldehyde into Schiff base, respectively, followed by reduction, Nitrosation or formylation in the system. 12 compounds were found to be effective in the initial screening of the pathogenicity of the P. falciparum-An. Anopheles system, in which 2,4-diamino 5 - [(3 ’, 4’- dichlorobenzylidene) - Amino] pyrimidine (compound V_3) and 2,4-diamino-5 - [(4’-bromobenzyl) -N -nitroamino] pyrimidine (compound VII_4) A total of three days, mice can be protected, did not see the blood parasite.