摘要
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。
Ten 4methyl5substitutedphenoxy6methoxy8[(1ethyl4amino)butylamino] quinolines (10a～j) have been synthesized and evaluated preliminarily for both suppressive and causal prophylactic antimalarial activities. The results of preliminary screening test showed that three of these compounds exhibited significant activity against Plasmodium yoelii in mice, among which 10c was 4～8 times as effective as primaquine. Moreover, 10c was superior to primaquine in suppressive test against Plasmodium berghei K173 strain in mice. On the basis of ED50 and ED90, 10c was about 2 times as active as primaquine. Most of other compounds showed similar activity and the minority of them exhibited lower activity compared with primaquine.
出处
《药学学报》
CAS
CSCD
北大核心
1998年第3期194-200,共7页
Acta Pharmaceutica Sinica
关键词
8-氨基喹啉
伯氨喹衍生物
抗疟活性
8Aminoquinolines
4,5Disubstituted analogues of primaquine
Antimalarial activity
