A number of 3-(dialkylamino)-1H-pyrimido[1,2-a]quinolin-1-ones 3 and 2-(dialkylamino)-4H-pyrimido[2,1-a]isoquinolin-4-ones4 were prepared by treating the corresponding chloro derivatives with an excess of dialkylamines. The highest in vitro antiplatelet activity was obtained when the dialkylamino substituent was 1-piperazinyl (compounds 3g and 4e). The novel 2-(1-piperazinyl)-4H-pyrido[1,2-a]pyrimidin-4-one2a was also prepared by an analogous procedure, which resulted in the most active compound towards all the platelet aggregation inducers used (ADP, collagen, A 23187). Moreover, some examples of 1-(dialkylamino)-3H-pyrimido[1,2-a]quinolin-3-ones5 and 4-(dialkylamino)-2H-pyrimido[2,1-a]isoquinolin-2-ones 6 were also obtained (together with negligible or lower amounts of the corresponding isomers 3 and 4, respectively) from the cyclocondensation of the appropriate ethylN,N -dialkylmalonamate/phosphorus oxychloride reagents 13 with 2-aminoquinoline or 1-aminoisoquinoline. These latter compounds showed a rather low antiplatelet activity.