| This study explores the design and synthesis of novel tri-imidazole derivatives and their corresponding metal chloride complexes. The tri-imidazole ligand was synthesized via a multi-component condensation reaction involving benzil, ammonium acetate, and salicylaldehyde derivatives. Coordination of this ligand with platinum(IV), palladium(II), nickel(II), and copper(II) chloride salts yielded a series of stable solid-state metal complexes. The structural architectures of the synthesized compounds were elucidated using a comprehensive suite of spectroscopic and analytical techniques, including UV–Visible, FT-IR, and 1H-NMR spectroscopy, alongside mass spectrometry, elemental analysis, magnetic susceptibility, and molar conductivity measurements. Metal content was precisely determined via Atomic Absorption Spectroscopy (AAS). Spectroscopic evidence confirmed that the ligand coordinates as a bidentate chelating agent. Geometric analysis revealed that the [L–Pt] complex adopts an octahedral configuration, whereas the [L–Pd], [L–Ni], and [L–Cu] complexes exhibit square planar geometries. The biological efficacy of the synthesized compounds was evaluated against selected microbial strains and cancer cell lines to assess their antibacterial, antifungal, and cytotoxic potential. The results demonstrated that the metal complexes possess significantly enhanced bioactivity compared to the free ligand. Notably, the platinum complex [L–Pt] exhibited superior biological performance, outperforming all other synthesized complexes. Furthermore, when compared to the clinical gold standard, Cisplatin, the [L–Pt] complex demonstrated higher potency, establishing it as the most effective antibacterial and anticancer agent in this study. These findings highlight the [L–Pt] complex as a promising candidate for the development of advanced metallotherapeutic drugs. |