Few vanadium metal complexes using substituted acetylacetones were synthesized, characterized and their biological activities were evaluated. The purpose of this investigation is twofold. Firstly, to evaluate the inhibitory properties of these vanadium metal complexes on enzyme PTP-1B. Secondly, to know the ease with which these metal complexes are being transported by transporting proteins like BSA. To synchronize these results, experiments on induced diabetic Wistar Rats were conducted. Molecular modeling studies were also performed to support the in vitro results. It has been shown by the kinetic studies that vanadium complexes are good inhibitors on PTP-1B enzyme. These complexes upon injecting have reduced the serum glucose levels to normal range in induced diabetic Wistar rats within 3 days of experiments. The order of glucose reducing properties of these metal complexes from different experiments is found to be the same. The vanadium ternary metal complex derived from 2,2,6,6-tetramethyl-3,5-heptanedione and imidazole as ligands is the best among the other metal vanadium complexes.