Original Article

Synthesis, toxicity and antimalarial effects of bispyroquine

Dao-xing Ren, Lan-sun Huang, Xian-yu Zheng, Jin-lin Sun, Rui-zhen Tang, Chang Chen, Jun-shi Chen, Shou-ping Yao


A new antimalarial agent was synthesized by introducing another pyrrolidine into amopyroquine to form 7-chlo-ro-4- (3',5'-di-pyrrolidin-l-y 1-methyl-4’-hyd roxy-phenyl) aminoquinoline, possessing dual pyrolidin-l-yl-methylphenolic side chain, named "bispyroquine" (M6407). It showed a strong schizontocidal activity against Plasmodium berghei and a low toxicity to mice. The therapeutic indices of bispyroquine and chloroquine were 37 and 9 by ig, 17.5 and l.3 by im, respectively. Hence bispyroquine is superior to chloroquine.

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