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Three new complexes formulated as [Cu(mbmb) 2 Cl 2 ] (1), [Cu(mbmb) 2 (NO 3) 2 ] (2), and [Zn(mbmb) 2 Cl 2 ] (3) (mbmb = 1-[(2-methyl-1H-benzoimidazol-1-yl)methyl]-1H-benzotriazole) have been synthesized and characterized. Complexes 1 – 3 showed mononuclear structures and the central metal ions of complexes 1 – 3 exhibited a four-coordinated environment. We evaluated the antioxidant activity against DPPH and antidiabetic activity against α-amylase of complexes 1 – 3 and ligand (mbmb) in vitro. The results of DPPH free radical scavenging assay showed that complexes 1 and 2 exhibited higher antioxidant activity among the synthesized compounds and their IC 50 values were 43.72 μg/mL and 43.76 μg/mL, respectively. The IC 50 values in vitro antidiabetic studies of complex 1 (0.74 mg/mL) and complex 2 (1.00 mg/mL) were much smaller than those of standard acarbose (2.34 mg/mL) and the ligand mbmb (39.87 mg/mL), which showed effective inhibition on α-amylase. Additionally, the solid-state fluorescent properties of these three complexes and ligand mbmb were investigated at room temperature. Unlabelled Image • Three new benzimidazole-based Cu(II)/Zn(II) complexes 1 – 3 were synthesized. • The structure of complexes 1 – 3 was characterized adequately by X-ray study. • The antioxidant activities of complexes 1 – 3 were evaluated by the DPPH free radical scavenging assay. • The antidiabetic activities against α-amylase of complexes 1 – 3 were investigated in vitro. [ABSTRACT FROM AUTHOR]