伯氨喹类似物的合成及其抗鼠疟活性
SYNTHESIS OF PRIMAQUINE ANALOGUES AND THEIR ANTIMALARIAL ACTIVITY IN MICE
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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 Plasmodium yoeli 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 Plasmodium berghei 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。Abstract: Ten 4-methyl-5-substitutedphenoxy-6-methoxy-8-(1-ethyl-4-amino)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.
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