论文部分内容阅读
本文报道了6个4-甲基-5取代苯氧基-6-甲氧基-8-(1-甲基-4-氨基丁氨基)喹啉(Ⅲ)的合成。除Ⅲ_3外,所有化合物对鼠疟P.berghei的抑制性治疗作用和对鼠疟P.yoelii的病因性预防作用均优干伯喹,其中以Ⅲ_1最强。Ⅲ_1口服治疗作用的SD_(50)和SD_(90)分别为0.65 mg/kg和1.60 mg/kg,口服预防作用的最小有效剂量(MED)和最小完全有效剂量(MFAD)分别为2.5mg/kg和5.0 mg/kg。对这类化合物的根治作用和毒性试验正在进行中。
This paper reports the synthesis of six 4-methyl-5-substituted phenoxy-6-methoxy-8- (1-methyl-4-aminobutylamino) quinoline (Ⅲ) In addition to Ⅲ_3, all compounds inhibit the therapeutic effect of P. berghei against P. mallei and the etiological prophylaxis against P. yoelii was predominantly benzalkonium, with the highest concentration being Ⅲ_1. The SD_ (50) and SD_ (90) of oral treatment of Ⅲ_1 were 0.65 mg / kg and 1.60 mg / kg respectively. The minimum effective dose (MED) and minimum effective dose (MFAD) of oral preventive effect were 2.5 mg / kg And 5.0 mg / kg. Radical effects and toxicity testing of such compounds are underway.