8-[(1-烷基-4-氨基丁基)氨基]-6-甲氧基-4-甲基喹啉的合成及其抗疟活性
Synthesis and antimalarial activity of 8-[(1-alkyl-4-aminobutyl)amino]-6-methoxy-4-methylquinolines.
作者信息
Yan S J, Chien P L, Cheng C C
出版信息
J Med Chem. 1981 Feb;24(2):215-7. doi: 10.1021/jm00134a019.
PMID:7205891
Abstract
Three analogues of the causal prophylactic antimalarial primaquine were prepared and their antimalarial activity was evaluated. 8-[(1-Ethyl-4-aminobutyl)amino]-6-methoxy-4-methylquinoline (2a) demonstrated activity against Plasmodium berghei in mice at 20 mg/kg, with all animals cured at 320 mg/kg, and is without toxicity at 640 mg/kg. It also possessed outstanding causal prophylactic activity against Plasmodium cynomolgi in rhesus monkeys at very low dosages.
摘要
制备了三种因果性预防抗疟药伯氨喹的类似物，并评估了它们的抗疟活性。8-[(1-乙基-4-氨基丁基)氨基]-6-甲氧基-4-甲基喹啉(2a)在20mg/kg剂量时对小鼠体内的伯氏疟原虫显示出活性，在320mg/kg时所有动物均被治愈，且在640mg/kg时无毒性。它在非常低的剂量下对恒河猴体内的食蟹猴疟原虫也具有出色的因果性预防活性。
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