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自五十年代开始,常用的抗疟药物对恶性疟原虫株陆续产生耐药性。迫切需要寻找新结构类型的抗疟药,特别是病因性预防和根治药物。早在三十年代就发现脒类化合物(Ⅰ)具有抗疟作用,但效果不够理想。1980年Sleiger等报道4′,6-二脒基-2-苯基吲哚(DAPI,Ⅱ)对伯氏鼠疟原虫(Plasmodium berghei)有较 X=-CH=CH-,-C≡C-,-O(CH_2)_5O-,-O-好作用。我们合成后,并用约氏鼠疟原虫(P.yoelii)-斯氏按蚊(Anopheles stephensi)系统鼠疟模型进行了病因性预防试验,结果表明:口服效果差,静脉注射或皮下注射效果较好,5
Since the 1950s, commonly used antimalarial drugs have developed resistance to P. falciparum strains. There is an urgent need to find new types of antimalarial drugs, especially etiological prevention and cure. As early as 1930s, it was found that amidine compound (I) has anti-malarial effect, but the effect is not satisfactory. In 1980, Sleiger et al. Reported that 4 ’, 6-diamidino-2-phenylindole (DAPI, II) has more X = -CH = CH-, -C≡C- , -O (CH 2) _5O -, -O- good effect. After our synthesis, we used the P. yoelii-Anopheles stephensi murine malaria model to conduct a causative prophylaxis trial. The results showed that oral administration was poor and intravenous or subcutaneous injection was effective 5