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寻找高效低毒的间日疟根治药是当前抗疟药研究中的一项重要课题。自伯喹问世30余年以来,至今尚无可以代替它的理想药物。Coatney等曾指出,某些5-取代苯氧基-6-甲氧基-8-氨基喹啉类化合物,比相应的5位上无取代基的同源物具有更强的抗疟活性和较低的毒性。近年来Chen等和Tanabe等报道,某些5-取代苯氧基伯喹衍生物的毒性低于伯喹,其中5-对氟苯氧基伯喹的抗疟作用略优于伯喹。作者于1979年已合成此化合物(Ⅷ_t)。其对红内期伯氏原虫(Plasmodium berghei)的作用明显较伯喹强,对鼠疟的病因性预防作
Looking for high efficiency and low toxicity of vivax malaria drug is an important issue in the current antimalarial research. Since the advent of Beauquat more than 30 years, so far no ideal medicine to replace it. Coatney et al. Have pointed out that certain 5-substituted phenoxy-6-methoxy-8-aminoquinolines have stronger anti-malarial activity than the corresponding homologues at the 5-position without substituents Low toxicity. In recent years, Chen et al. And Tanabe et al. Reported that the toxicity of some 5-substituted phenoxyquacoquin derivatives is lower than that of primaquine, and the antimalarial activity of 5-p-fluorophenoxyquine is slightly better than that of primaquine. The author has synthesized this compound in 1979 (Ⅷ_t). Its effect on Plasmodium berghei was significantly stronger than that of norcquat, and its preventive effect on the pathogenesis of murine malaria