Abstract: In order to search for potential agents acting on nervous system, fourteen analogues of 4-hydroxy-3-(3-methyl-2-butenyl)-2-quinolone (Ⅳ,Ⅴ) were synthesized by the cyclization of substituted arylamines and diethyl 3-methyl-2butenyl malonate. Five related compounds of Ⅵ and Ⅶ were prepared similarly. In preliminary test in mice all these compounds, except Ⅵ, showed analgesic, anticonvulsant or central depressant activities on the nervous system. Further pharmacological studies on these compounds are in progress.