合成了咯萘啶(Ⅰ)的有关化合物Ⅱ～Ⅴ,以探讨抗疟药咯萘啶化学结构中母环1位上氮杂原子及吡咯烷基Mannich碱侧链的存在,对该化合物抗疟作用的关系。经对有抗药性的疟原虫体内试验,合成的有关化合物Ⅱ～Ⅴ以及抗疟药氯喹和阿的平等的抗疟作用,均不如咯萘啶。提示上述氮杂原子及Mannich碱铡链的存在,对咯萘啶的抗疟作用,起着重要的和不可缺少的作用。 The related compounds Ⅱ ~ Ⅴ of pyronaphthyridine (Ⅰ) were synthesized to investigate the existence of side chain of nitrogen atom and pyrrolidinyl Mannich base at the 1-position of the parent ring of the antimalarial drug pyrrole, The role of the relationship. The antimalarial activity of the synthetic compounds II-V and chloroquine and anti-malarial drugs chloroquine and arabinoside was not as good as that of pyronaridine after in vivo testing against resistant plasmodium. It is suggested that the existence of the above nitrogen heteroatoms and Mannich base chain plays an important and indispensable role in the anti-malarial action of pyronaridine.