4,5-二取代伯氨喹类似物作为潜在的抗疟药。
4,5-Disubstituted primaquine analogues as potential antimalarial agents.
作者信息
Carroll F I, Berrang B D, Linn C P
出版信息
J Med Chem. 1986 Sep;29(9):1796-8. doi: 10.1021/jm00159a042.
PMID:3746825
Abstract
Three 4,5-disubstituted primaquine analogues were synthesized and evaluated for radical curative activity against Plasmodium cynomolgi in rhesus monkeys. One of the compounds showed moderate activity; however, none of the three compounds were as active as the lead compounds 5-methoxy-4-methylprimaquine and 4-(methoxy-methyl)-5-[m-(trifluoromethyl)phenoxy]primaquine.
摘要
合成了三种4,5-二取代伯氨喹类似物，并在恒河猴中评估了它们对食蟹猴疟原虫的根治活性。其中一种化合物表现出中等活性；然而，这三种化合物均不如先导化合物5-甲氧基-4-甲基伯氨喹和4-(甲氧基甲基)-5-[间-(三氟甲基)苯氧基]伯氨喹活性高。
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