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本文报道α-(烷氨基甲基)-7-溴-4-芴甲醇Ⅰ和α-(烷氨基甲基)-2,7-二氯-4-芴甲醇Ⅱ的合成。动物筛选的初步结果表明,这两类化合物均有一定的抗鼠疟作用。Ⅱ类化合物的抗疟作用比Ⅰ类化合物的强,Ⅱ类中的大多数化合物用25mg/kg的剂量即能抑制感染伯氏鼠疟原虫株(Plasmodium berghei berghei NK 65)小白鼠的原虫血症,其中Ⅱ_g,Ⅱ_b和Ⅱ_i用5mg/kg的剂量也能达到完全抑制。
This paper reports the synthesis of α- (alkylaminomethyl) -7-bromo-4-fluorenemethanol Ⅰ and α- (alkylaminomethyl) -2,7-dichloro-4-fluorenemethanol II. The preliminary results of animal screening show that both compounds have some anti-malarial effects. The antimalarial activity of class II compounds was stronger than that of class I compounds and most of the compounds in class II were able to inhibit protozoalosis in mice infected with Plasmodium berghei berghei NK 65 mice at a dose of 25 mg / kg , Of which Ⅱ_g, Ⅱ_b and Ⅱ_i with 5mg / kg dose can achieve complete inhibition.