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本文报道了22个7-三氟甲基和2-甲基-7-三氟甲基氨酚喹类似物的合成。用伯氏疟原虫(plasmodium berghei)ANKA正常株感染小鼠作抑制性治疗试验,在剂量为(10 mg/kg)/d×4和(20 mg/kg)/d×4时,有11个化合物(Ⅰ_(1～9),Ⅱ_3和Ⅱ__6)对疟原虫完全抑制。其中3个化合物(Ⅰ_2,Ⅰ_6和Ⅰ_7)在剂量为(5 mg/kg)/d×4时,就能对原虫完全抑制。12个化合物(Ⅰ_(1～10),Ⅱ_3和Ⅱ_6)用伯氏疟原虫ANKA抗氯喹株感染小鼠作治疗试验,剂量为(20 mg/kg)/d×4,2个化合物(Ⅰ_4和Ⅱ_3)在受试的5只小鼠中,原虫完全被抑制的鼠分别为3和4只,用相同剂量的对照药物盐酸氨酚喹治疗,原虫仍为阳性。
This paper reports the synthesis of 22 analogues of 7-trifluoromethyl and 2-methyl-7-trifluoromethylquinolinol. Infection-inhibiting mice were challenged with normal ANKA strain of plasmodium berghei at a dose of (10 mg / kg) / dx4 and (20 mg / kg) / dx4 and 11 The compounds (Ⅰ_ (1-9), Ⅱ_3 and Ⅱ_6) completely inhibited Plasmodium. Three of these compounds (Ⅰ_2, Ⅰ_6 and Ⅰ_7) were able to completely inhibit protozoa at a dose of 5 mg / kg / d × 4. Twelve compounds (Ⅰ_ (1-10), Ⅱ_3 and Ⅱ_6) were used to treat mice infected with Plasmodium berghei ANKA against chloroquine, and the dose was 20 mg / kg / d × 4 and 2 compounds (Ⅰ_4 and Ⅱ_3) Among the 5 mice tested, 3 and 4 mice whose protozoa were completely inhibited were still positive with the same dose of the control drug paracetamol hydrochloride.