This article presents structural characteristic andin vivoantihyperglycemic activities of three new homobimetallic Zn(II) dithiocarbamates (1–3) with general formula [ZnL2]2, where L is 4-(3-methoxyphenyl)piperazine-1-carbodithioate (1), 4-(4-methoxyphenyl)piperazine-1-carbodithioate (2) and 4-benzhydrylpiperazine-1-carbodithiaoate (3). These complexes have been characterized by elemental analysis, FT-IR, multinuclear NMR (1H and13C), and X-ray single crystal analysis. The latter technique has confirmed the homobimetallic nature of1and2in which Zn ions are linked via sulfurs to form a four-membered ring Zn2S2. Non-covalent intermolecular interactions give a supramolecular ladder-like zigzag chain (1) and layered structure (2). The antihyperglycemic activities revealed that the blood glucose lowering ability follows the trend: glibenclamide (83.0 mg dL−1) > 3(97.6 mg dL−1) > 2(100.4 mg dL−1) > 1(141.4 mg dL−1). [ABSTRACT FROM AUTHOR]