论文部分内容阅读
为寻找高效低毒的8-氨基喹啉类抗疟新药,用1-[(3-氯丙基)-4-(氨基烷基)]哌嗪在三乙胺存在下与环上取代的8-氨基喹啉缩合,合成了一系列 N-哌嗪基烷基取代的8-氨基喹啉类化合物(1～20)。其中多数对鼠伯氏疟原虫感染的抑制性治疗均具一定的活性,在20mg/kg×4d 的剂量下,化合物1,6,10和19的原虫抑制率为100%。在病因性预防筛选中,化合物1,18和19可使感染约氏疟原虫子孢子的实验鼠全部得到保护。化合物1在10mg/kg×3d 的剂量下仍有4/5的实验鼠保持阴性,仍比伯喹为优。
In order to search for an effective and low toxic 8-aminoquinoline anti-malaria drug, the title compound was synthesized with 1 - [(3-chloropropyl) -4- (aminoalkyl)] piperazine in the presence of triethylamine - aminoquinoline condensation, a series of N-piperazinyl alkyl-substituted 8-aminoquinolines (1-20) were synthesized. Most of them inhibited the Plasmodium berghei infection with certain activity, and the protozoal inhibitory rates of compounds 1, 6, 10 and 19 were 100% at 20 mg / kg × 4d. Compounds 1, 18 and 19 all protected the mice infected with P. yohii sporozoites from etiologic prevention screening. Compound 1 remained 4/5 of the experimental mice at a dose of 10 mg / kg by 3 d, still less than primaquine.