Abstract: In order to search for new antimalarial agents superior to shangrolin, a series of 4-N-substituted quinazoline derivatives were prepared from quinazolones bearing various substituents. Antimalarial screening results showed that 2-methyl-4-3', 5'-bis -(N-pyrrolidinyl)methyl-4'-hydroxyanilino quinazoline (Compound 13) and 6,7,-methylenedioxy-4-3'-(N-pyrrolidinyl) methyl-4'-hydroxyanilino quinazoline (Compound 16) were more active than Shangrolin against P. berghei in mice.