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前文报道2-特丁氨甲基-4-(7′-氯-4′-喹啉氨基)-5,6,7,8-四氢-1-萘酚盐酸盐对伯氏鼠疟原虫敏感株的作用较强,但对抗氯喹株有一定的抗性,在一些抗疟药中单边或双边取代的氨基苯酚侧链对抗疟作用也有一定的影响。Ohnmach等报道的甲氟喹,在其母核的2位和8位各为三氟甲基取代,与同类化合物相比,有较强的抗疟作用,并与氯喹无交叉抗药性,已在临床试用。因此,我们用三氟甲基代替喹啉核7位上的氯原子,并在喹啉核的4
It has been reported previously that 2-tebutamino-4- (7’-chloro-4’-quinolinolamino) -5,6,7,8-tetrahydro- Sensitive strains have stronger effects, but have some resistance to chloroquine resistant strains. In some antimalarial drugs, unilateral or bilateral substitution of aminophenol side chains also has an impact on the anti-malarial effect. The mefloquine reported by Ohnmach et al., Was substituted with trifluoromethyl at the 2 and 8 positions of its parent nucleus. Compared with similar compounds, mefloquine showed strong antimalarial activity and no cross-resistance with chloroquine. Clinical trial. Therefore, we use trifluoromethyl instead of the chlorine atom on the quinoline nucleus 7, and in the quinoline nucleus 4