Meng X Y, Liu J Q, Zhang X P, Chen X H, Yu A Z, Dai Z R
Shanghai Institute of Pharmaceutical Industry.
Yao Xue Xue Bao. 1994;29(4):261-7.
The title compounds were synthesized by condensation of 5-fluoro- 2, 4, 6-triaminoquinazoline (6a) with various substituted benzaldehydes to produce the corresponding Schiff bases, followed by reduction. II and III were obtained by formylation and nitrosation of I, respectively, IV were obtained by reduction of II. Primary screening for suppressive therapeutic effects against P. berghei in mice showed that six of the twenty-two compounds produced 100% suppression when administered orally at a dose of 1 mg.kg-1. All compounds exhibited potent activity against L1210 cell in vitro. Among them I4 was more active than MTX. A number of compounds showed moderate activities against Diplococcus pneumoniae in vitro tests.
通过将5-氟-2,4,6-三氨基喹唑啉（6a）与各种取代的苯甲醛缩合制备相应的席夫碱，然后进行还原反应，合成了标题化合物。分别通过对I进行甲酰化和亚硝化反应得到II和III，通过对II进行还原反应得到IV。对小鼠伯氏疟原虫抑制治疗效果的初步筛选表明，二十二种化合物中有六种在以1mg·kg-1的剂量口服给药时产生了100%的抑制作用。所有化合物在体外对L1210细胞均表现出强效活性。其中I4比甲氨蝶呤更具活性。许多化合物在体外试验中对肺炎双球菌表现出中等活性。
