Abstract: In searching for new antimalarial agents ten new compounds of 2,4-diamino-6-N-(substituted benzyl)-N-(substituted aminomethyl)-amino-quinazoline have been synthesized. Preliminary screening results showed that only one (Ⅳ₆) of these compounds displayed a slight degree of antimalarial activity against plasmodium berghei in mice. The intermediate compound (Ⅰ₂) showed suppressive effect on plasmodium berghei in mice and prophylactic activity against plasmodium gallinaceum in chicken.