Raynes K, Galatis D, Cowman A F, Tilley L, Deady L W
Chemistry School, La Trobe University, Bundoora, Victoria, Australia.
J Med Chem. 1995 Jan 6;38(1):204-6. doi: 10.1021/jm00001a026.
A new type of bisquinoline antimalarial, in which the basic side chain of chloroquine is retained, has been evaluated. Nine bisamides were prepared from aliphatic diacids with 6-amino- and 8-amino-((4-(diethylamino)-1-methylbutyl)amino)quinoline, and screened against chloroquine-sensitive and -resistant strains of Plasmodium falciparum in vitro. The resistance indices for all compounds were lower than for chloroquine. The position of attachment and length of the linker chain markedly affected activity. The most active (IC50 = 120 nM against the chloroquine-resistant FAC8 strain) was the -(O)C(CH2)4C(O)- linked 8-amino compound.
一种新型的双喹啉抗疟药已被评估，该药物保留了氯喹的碱性侧链。用脂肪族二酸与6-氨基-和8-氨基-((4-(二乙氨基)-1-甲基丁基)氨基)喹啉制备了9种双酰胺，并在体外针对氯喹敏感和耐药的恶性疟原虫菌株进行了筛选。所有化合物的耐药指数均低于氯喹。连接位置和连接链的长度对活性有显著影响。活性最高的（对氯喹耐药的FAC8菌株的IC50 = 120 nM）是-(O)C(CH2)4C(O)-连接的8-氨基化合物。
