[Synthesis of 4-methyl-5-substituted phenoxy-primaquine analogues and preliminary evaluation on their antimalarial...

On basis of our previous work, seven 4-methyl-5-substituted phenoxy-6-methoxy-8-(1-methyl-4-amino-butylamino)-quinolines (II2-8) were synthesized and their antimalarial activities were preliminarily evaluated. The target compounds were prepared from 2-nitro-4-methoxy-5-bromo-acetanilide as previously described. The structures of II2-8 and all of the unknown intermediates were confirmed by elementary and spectral analyses. Preliminary biological evaluation revealed that all of II2-8 exhibited significant blood schizonticidal activity and were 4-8 times as effective as primaquine in causal prophylactic test in mice.