Nickel P, Barnickel H, Preissinger L, Fink E, Dann O
Arzneimittelforschung. 1978;28(3):367-72.
19 derivatives, 10 a--t, of 6-(4-diethylamino-1-methylbutylamino)-5,8-dimethoxyquinoline (1a) with alkoxy-, hydroxy-, and methylmercapto substituents in 4- and/or 2-position were synthesized with the aim of studying the influence of these substituents on antimalarial activity and toxicity of 1a. The alkoxy derivatives of 1a are highly active against P. vinckei (mouse). The 2- and 4-hydroxy derivatives, 10 l and 10 m, are inactive.
合成了6-(4-二乙氨基-1-甲基丁基氨基)-5,8-二甲氧基喹啉(1a)在4-和/或2-位带有烷氧基、羟基和甲硫基取代基的19种衍生物,即10种a - t,目的是研究这些取代基对1a抗疟活性和毒性的影响。1a的烷氧基衍生物对文氏疟原虫(小鼠)具有高活性。2-和4-羟基衍生物,即10 l和10 m,没有活性。