Objectives This study was done to synthesize a novel Zn(II)‐gallic acid complex with improved antidiabetic and antioxidative properties. Methods The complex was synthesized and characterized using Fourier Transform Infrared (FT‐IR) and 1H NMR. Cytotoxicity was evaluated using Chang liver cells and L6 myotubes. Radical scavenging and Fe3+‐reducing, as well as α‐glucosidase, α‐amylase and glycation inhibitory properties were measured. Glucose uptake was measured in L6 myotubes, while the complex was docked against glucose transporter type 4 (GLUT‐4) and protein kinase B (PKB). Key findings Analysis showed that complexation occurred through a Zn(O4) coordination; thus, the complex acquired two moieties of gallic acid, which suggests why complexation increased the DPPH (IC50 = 48.2 µm) and ABTS (IC50 = 12.7 µm) scavenging and α‐glucosidase inhibitory (IC50 = 58.5 µm) properties of gallic acid by several folds (5.5, 3.6 and 2.7 folds; IC50 = 8.79, 3.51 and 21.5 µm, respectively). Zn(II) conferred a potent dose‐dependent glucose uptake activity (EC50 = 9.17 µm) on gallic acid, without reducing the viability of L6 myotubes and hepatocytes. Docking analysis showed the complex had stronger interaction with insulin signalling proteins (GLUT‐4 and PKB) than its precursor. Conclusions Data suggest that complexation of Zn(II) with gallic acid resulted in a complex with improved and multi‐facet antioxidative and glycaemic control properties.