Liu J Q, Xu X G, Chen X H, Yu A Z, Dai Z R, Zhang X P
Shanghai Institute of Pharmaceutical Industry.
Yao Xue Xue Bao. 1991;26(11):821-8.
Title compounds were synthesized by condensation of 5-chloro-2,4,6-triaminoquinazoline (8) with various substituted benzaldehydes to produce the corresponding Schiff bases, followed by reduction with NaBH4, II and III were obtained by formylation or nitrosation of I respectively. Primary screening for suppressive therapeutic effects against P. berghei in mice showed that eight of the twelve compounds produced 100% suppression when administered orally at dose of 20 mg/kg. The results against L1210 Leukemia cell and B16 melanoma cell in vitro exhibited potent inhibition. Among them four compounds were more active than MTX and SIPI 759. Further work is in process. Antibacterial tests in vitro showed that a number of compounds possessed moderate activities against Diplococcus pneumoniae.
通过将5-氯-2,4,6-三氨基喹唑啉（8）与各种取代的苯甲醛缩合制备相应的席夫碱，从而合成标题化合物，随后用NaBH4还原，分别通过I的甲酰化或亚硝化得到II和III。对小鼠伯氏疟原虫抑制治疗效果的初步筛选表明，当以20mg/kg的剂量口服给药时，十二种化合物中的八种产生了100%的抑制作用。对L1210白血病细胞和B16黑色素瘤细胞的体外实验结果显示出强效抑制作用。其中四种化合物比甲氨蝶呤和SIPI 759更具活性。进一步的工作正在进行中。体外抗菌试验表明，许多化合物对肺炎双球菌具有中等活性。
