A novel series of antimony (V) complexes with the hydroxypyranone and hydroxypyridinone ligands were synthesized and characterized by HNMR, FT-IR and electron spin ionization mass spectroscopic (ESI-MS) techniques. The synthesis process involved protection of hydroxyl group followed by the reaction of the intermediate with primary amines and finally deprotection. All compounds were evaluated for activities against the amastigote and promastigote forms of . Most of the synthesized compounds exhibited good antileishmanial activity against both forms of . IC values of the most active compounds; , and , after 24, 48 and 72 h against amastigote model were 15, 12.5 and 5.5 μg/mL, respectively. , and inhibited the promastigote form of parasite after 24, 48 and 72 h with IC values of 10, 2 and 1 μg/mL, respectively.