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根据5-(对-氟苯氧基)-6-甲氧基-8-(4-氨基-1-甲基-丁氨基)喹啉(Ⅰ_1)(表1)对猴疟原虫(Plasmodium cynomolgi)的作用略优于伯喹而毒性较低的报道,合成了化合物Ⅰ_1(代号M7844),同时还合成了衍生物5-取代苯氧基-6-甲氧基-8-(4-取代氨基-1-甲基丁氨基)喹啉(Ⅰ_(3～17))(表1)以及其同分异构体5-取代苯氧基6-甲氧基-8-(5-取代氨基戊氨基)喹啉(Ⅱ_(13～28))(表2)。药理研究证明化合物Ⅰ_(1～7、Ⅰ_(16)及Ⅱ_(18)等对鼠疟P.yoelii均有不同程度的作用。化合物Ⅰ_1(M7844)的毒性甚低,对小鼠的毒性比磷酸伯喹低20余倍,对家兔的溶血反应也明显低干伯喹。但在相同剂量下,对猴疟P.cynomolgi的作用不及伯喹。对鼠疟红前期的作用比伯喹低4～5倍。
Plasmodium cynomolgi was isolated from 5- (p-fluorophenoxy) -6-methoxy-8- (4-amino-1-methylbutylamino) quinoline (Table 1) Was slightly superior to primaquine and its toxicity was relatively low. Compound Ⅰ_1 (codename M7844) was synthesized and the derivative 5-substituted phenoxy-6-methoxy-8- (4-substituted amino- 1-methylbutylamino) quinoline (I_ (3-17)) (Table 1) and its isomer 5-substituted phenoxy 6-methoxy- 8- (5-substituted aminopentylamino) Quinoline (Ⅱ_ (13 ~ 28)) (Table 2). Pharmacological studies showed that compounds Ⅰ_ (1-7), Ⅰ_ (16) and Ⅱ_ (18) had different effects on P. yoelii.Compound I_1 (M7844) had low toxicity and toxicity to mice than that of phosphoric acid Berberine is more than 20 times lower, and the haemolytic response to rabbits is also significantly lower than that of benzalkonium, but the effect on P.cynomolgi is not as good as that of primaquine at the same dose, ~ 5 times.