论文部分内容阅读
报道１０个４甲基５取代苯氧基６甲氧基８［（１乙基４氨基）丁氨基］喹啉（１０ａ～ｊ）的合成及其抗疟活性。鼠疟初筛结果表明，有３个化合物对鼠疟Ｐｌａｓｍｏｄｉｕｍｙｏｅｌｉ的病因性预防作用较强，其中１０ｃ的活性可达伯氨喹的４～８倍；同时，１０ｃ也有较强的杀血液裂殖体活性，对鼠疟Ｐｌａｓｍｏｄｉｕｍｂｅｒｇｈｅｉ的抑制性治疗作用以ＥＤ５０和ＥＤ９０计算，为伯氨喹的２倍，其余多数化合物活性与伯氨喹相当，少数不如伯氨喹。
Reported the synthesis of 10 4-methyl-5-substituted phenoxy-6-methoxy-8- [(1-ethyl- 4-amino) butylamino] active. The results of the preliminary screening of murine malaria showed that three compounds had a strong preventive effect on Plasmodium yoelii, of which the activity of 10c was 4-8 times higher than that of primaquine. Meanwhile, 10c also had a strong schizonts The inhibitory therapeutic effect on Plasmodiumberghei against Plasmodiumberghei was twice as that of primaquine calculated with ED50 and ED90. The rest of the compounds showed comparable activities to primaquine, with fewer than primaquine.