Dann O, Nickel P, Hölzel W R, Lisson K G, Fink E, Steuding W
Arzneimittelforschung. 1982;32(9):1016-23.
3 derivatives 2g--i of 6-(4-diethylamino-1-methylbutylamino)-4-methoxy-2-methylquinoline and 6 derivatives 2k--p of 6-(4-diethylamino-1-methylbutylamino)-2,4-dimethylquinoline were synthesized with variations of substituents in positions 5 and 8 (--H, --OH, --OCH3, --CH3, --Cl) with the aim of studying the influence of these substituents, which facilitate, complicate or prevent oxidation to o- and (or) p-quinones, on antimalarial activity and toxicity. One methoxy group is necessary for activity against Plasmodium vinckei in position 5 or 8, no substituent that prevents oxidation is allowed in para position to this methoxy group.
合成了6-(4-二乙氨基-1-甲基丁基氨基)-4-甲氧基-2-甲基喹啉的3种衍生物2g-i以及6-(4-二乙氨基-1-甲基丁基氨基)-2,4-二甲基喹啉的6种衍生物2k-p，其5位和8位（-H、-OH、-OCH₃、-CH₃、-Cl）带有不同取代基，目的是研究这些有助于、使复杂化或阻止氧化成邻醌和（或）对醌的取代基对抗疟活性和毒性的影响。5位或8位上的一个甲氧基对于抗文氏疟原虫的活性是必需的，在该甲氧基的对位不允许有阻止氧化的取代基。
