Abstract: In an effort to modify the structure of edulinine so to seek compounds exhibiting higher potency toward inhibition of central nervous system, we designed and synthesized several analogous compounds: 2-methoxy-3-(3-methyl-2-butenyl)-4-oxo-4 H-pyrido 1, 2-a pyrimidine (Ⅳ), 4-methoxy-3-(3-methyl-2-butenyl)-2-oxo-2H-pyrido1, 2-apyrimidine (Ⅴ), 2-methoxy-3-(2, 3-dihydroxy-3-methyl-1-butyl)-4-oxo-4H-pyrido1,2-a pyrimidine (Ⅵ), and 4-methoxy-3-(2,3-dihydroxy-3-methyl-1-butyl)-2-oxo-2H-pyrido1,2-apyrimidine(Ⅶ). Animal experiments revealed that compound (Ⅳ) has anticonvulsant activity, compounds (Ⅴ) and (Ⅵ) have far lower activity than compound (Ⅳ).