Two　series　of　novel　N-6　derivatives　of　8-azapurine　I　and　II　were　designed　as　antiplatelet　agents.　Series　I　and　II　were　N-6　amino　derivatives　and　N-6　hydrazone　derivatives　of　8-azapurine,　respectively.　The　compounds　were　synthesized　in　acceptable　yields　via　conventional　procedures,　including　nucleophilic　substitution,　diazotization,　and　amination　or　hydrazonation　with　amino　alcohol　and　4,6-dichloropyrimidine　as　starting　materials.　To　assess　the　ability　of　the　synthesized　compounds　as　antiplatelet　agents,　the　ADP-induced　platelet　aggregation　assay　of　Born　was　performed　both　in　vitro　and　in　vivo　using　ticagrelor　as　a　reference　control　substance.　The　analysis　of　the　structure-activity　relationship　and　molecular　docking　were　also　discussed　in　detail.　The　results　demonstrated　that　series　I　and　II　compounds　exhibited　antiplatelet　activity　in　vitro　and　IIh　was　the　most　active　compound　(IC50　=　0.20　mu　M)　among　the　target　compounds,　being　almost　4-fold　better　than　ticagrelor　(IC50　=　0.74　mu　M).　For　a　preliminary　assessment　of　the　safety　profile,　a　bleeding　test　(mouse　tail)　and　a　single-dose　toxicity　test　were　conducted.　The　use　of　compound　IIh　resulted　in　a　shorter　bleeding　time,　less　blood　loss　and　lower　acute　toxicity　compared　to　ticagrelor.　In　addition,　a　molecular　docking　study　was　performed　to　investigate　the　binding　capacity　and　binding　mode　between　IIh　and　P2Y(12).