2,4-二取代6-甲氧基-8-氨基喹啉类似物作为潜在抗寄生虫药物的合成
Synthesis of 2,4-disubstituted 6-methoxy-8-aminoquinoline analogues as potential antiparasitics.
作者信息
Carroll F I, Berrang B D, Linn C P
出版信息
J Med Chem. 1980 May;23(5):581-4. doi: 10.1021/jm00179a023.
PMID:6770089
Abstract
A series of 2,4-disubstituted 8-aminoquinoline analogues were synthesized and evaluated against Plasmodium berghei in mice and Leishmania donovani in hamsters. 8-[[6-(Diethylamino)hexyl]amino]-2-ethyl-6-methoxy-4-methylquinoline (8a) possessed significant activity against L. donovani. 2-Ethyl-4-methylprimaquine (7a) was evaluated against Plasmodium cynomolgi in rhesus monkey and found to have activity equal to that of primaquine.
摘要
合成了一系列2,4-二取代的8-氨基喹啉类似物，并在小鼠体内对伯氏疟原虫以及在仓鼠体内对杜氏利什曼原虫进行了评估。8-[[6-(二乙氨基)己基]氨基]-2-乙基-6-甲氧基-4-甲基喹啉（8a）对杜氏利什曼原虫具有显著活性。在恒河猴体内对2-乙基-4-甲基伯氨喹（7a）进行了食蟹猴疟原虫评估，发现其活性与伯氨喹相当。
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