STUDIES ON ANTIMALARIALS——Ⅲ. SYNTHESIS OF 2-(SUBSTITUTED STYRYL)-4-AMINO PYRIDINES

Nine 2-(substituted styryl)-4-amino, pyridines Ⅲ and three 2-(substituted styryl)-6-methyl-4-amino pyridines IV have been synthesized by condensation of 4-(4'-diethyl amino-1'-methyl amino)-2-methyl (or 2,6-dimethyl)-pyridine-with substituted aryl aldehydes.Preliminary results showed that compounds Ⅲ₂, Ⅲ₄ and Ⅲ₇ exhibited notable antimalarial activity against chloroquine-sensitive strain of P. berghei in mice at 6.25mg/kg after oral administration. Compound Ⅲ₇ can suppress parasitemia of mice infected with chloroquine-sensitive strain of P. berghei at 1.8 mg/kg subcutaneously. Among them Ⅲ₇ was the most active.