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作者等根据一些抗疟药的构效关系,合成了一种新化合物2-甲氧基-7-氯-10-[3′,5′-双(四氢吡咯次甲基)一4′-羟基苯胺基]苯骈[b]1,5-萘啶(Ⅰ),代号7351,定名咯萘啶。它对红内期裂殖体的作用显著,毒性低。之后,又合成了它的类似物Ⅱ,这些类似物大多数对鼠疟Plasmodiumberghei的红内期均具有不同程度的作用,其中Ⅱ_(1～6,9.10)等的作用与Ⅰ相当。对子孢子诱发感染的鼠疟P.yoelii的作用以化合物Ⅰ、Ⅱ_(1,3,5,6,9,10,12,15)等为最强,优于伯喹对照组。值得注意的是,这类化合物既对血液转种的鼠疟P.berghei具有显著的作用,同时对子孢子感染的鼠疟P.yoelii也具有显著的作用。
According to the structure-activity relationship of some anti-malarial drugs, the authors synthesized a novel compound 2-methoxy-7-chloro-10- [3 ’, 5’-bis (tetrahydropyrromethene- Hydroxyanilino] benzenesulfon [b] 1,5-naphthyridine (I), code 7351, designated pyronaphthyridine. Its role in the red mid-schizont significantly, low toxicity. Afterwards, its analog Ⅱ was synthesized, and most of these analogues had different degrees of effect on the red stage of Plasmodiumberghei. The effects of Ⅱ_ (1 ~ 6, 9.10) were similar to that of Ⅰ. The effect of P.yoelii on sporozoite-induced infection was the strongest in compound Ⅰ, Ⅱ_ (1,3,5,6,9,10,12,15), which was better than that of primaquine in control group. It is noteworthy that these compounds not only have a significant effect on blood-stained P. berghei, but also have a significant effect on sporozoite-infected P. yoelii.