Geary T G, Divo A A, Jensen J B
Department of Microbiology and Public Health, Michigan State University, East Lansing 48824-1101.
Trans R Soc Trop Med Hyg. 1987;81(3):499-503. doi: 10.1016/0035-9203(87)90175-1.
9 quinoline-containing antimalarials and the phenanthrene methanol halofantrine were tested in vitro against 6 strains of Plasmodium falciparum with known sensitivity to chloroquine. Sensitivity to chloroquine was not uniformly associated with sensitivity to mepacrine (quinacrine), halofantrine, SN-12108 or SN-6911 (3-methylchloroquine, sontochin). Amodiaquine was slightly less potent with chloroquine-resistant strains, whereas SN-12309 closely resembled chloroquine in the pattern of sensitivity. (Bis)desethylchloroquine was nearly as potent as chloroquine against chloroquine-sensitive strains but was about 10-fold less potent than the parent drug against chloroquine-resistant strains. 2 8-aminoquinolines, primaquine and pamaquine, were more potent against chloroquine-resistant than chloroquine-sensitive strains. The mutation(s) responsible for chloroquine resistance in P. falciparum greatly reduce(s) the sensitivity to a major metabolite of the drug but also generate(s) parasites which are more susceptible to a different class of drugs, the 8-aminoquinolines.
对9种含喹啉的抗疟药以及菲甲醇卤泛群进行了体外试验，以检测其对6株已知对氯喹敏感的恶性疟原虫的效果。对氯喹的敏感性与对米帕林（喹吖因）、卤泛群、SN - 12108或SN - 6911（3 - 甲基氯喹，孙托辛）的敏感性并非始终相关。阿莫地喹对耐氯喹菌株的效力略低，而SN - 12309在敏感性模式上与氯喹非常相似。双去乙基氯喹对氯喹敏感菌株的效力几乎与氯喹相同，但对耐氯喹菌株的效力比对母体药物低约10倍。两种8 - 氨基喹啉，伯氨喹和扑疟喹，对耐氯喹菌株的效力比对氯喹敏感菌株更强。恶性疟原虫中导致氯喹耐药的突变极大地降低了对该药物主要代谢物的敏感性，但也产生了对另一类药物8 - 氨基喹啉更敏感的寄生虫。
