本文报道标题化合物的合成及其抗疟、抗肿瘤和抗菌活性,该类化合物是以5-氯-2,4, 6-三氨基喹唑啉与各种取代苯甲醛缩合成相应的Schiff碱,然后经NaBH_4还原,再甲酰化或亚硝化制得.经对感染伯氏疟原虫(P.berghei)的鼠抑制性治疗筛选,有八个化合物剂量20mg/kg×4d时抑制率100%,Ⅰ_3,Ⅰ_4,Ⅲ_4三个化合物剂量5mg/kg×4d时抑制率在90%以上;体外抗肿瘤试验有4个化合物的活性优于MTX和SIPl759,以Ⅰ_4最佳。对L1210白血病细胞株的IC_(50)为2.20×10^(-9) m mol/L;经对18种常用菌株进行体外筛选,发现对肺炎双球菌(D.pneumoniae)有较好的活性。
\ 2Alkyl6oxo8fluoro9(4methylpiperazin1yl)6Himidazo(4,5,1ij)quinoline5carboxylic acids (2Ab～2Ae) were prepared by condensation of ethyl 6fluoro7(4methylpiperazin1yl)8amino1,4dihydro4oxo3quinolinecarboxylate (5A) with the aliphatic acids in PPA. Other target compounds 2Af～2Ah, 2Bc, 2Cc, 2Aa～2Da, 2Bi and 2Ci were prepared by the condensation of 6fluoro7nitrogencontaining heterocycle8amino1,4dihydro4oxo3quinolinecarboxylic acids (9A～9D) with the corresponding acids in PPA or with ethyl orthoformate or by the diazotisation of 9B and 9C, respectively. Only 2Ab and 2Ac showed moderate antibacterial activity in in vitro test.
