Stilbenes are compounds found in numerous medicinal plants and food products with some known biological and even antileishmanial activity. This paper describes the preparation of Aza-stilbene derivatives and their in vitro biological activities against Leishmania species. Most of the compounds with hydroxyl groups ( 2a , 2b , 2d , 2e and 2f ) showed interesting results against three Leishmania species tested. Compound 2f showed the best activity against intracellular forms of L. amazonensis , with IC50 of 7.48 μM, very similar when compared to reference drug Miltefosine. It not possible associate NO production with leishmanicidal activity for all aza-stilbene derivatives. It is noteworthy that none of compounds tested showed cytotoxicity against macrophages.