In the present work, a new series of compounds containing 1,2,3-triazole and 2-pyrazoline moieties in the same matrix was synthesized via a multistep synthetic route. The synthesized compounds were characterized by FT-IR, 1HNMR and 13C NMR spectra. The target compounds and their precursors were screened in vitro for their α-amylases inhibitory activity. The preliminary activity results revealed that all the tested compounds displayed an inhibition activity ranged from moderate to high depending on their structures and concentrations compared to ascorbose as a standard drug.