Synthesis And Bioactivity Of Metal Complexes As DPP-IV Enzyme Inhibitors

A series of novel metal complexes were designed and synthesized as DPP-IV inhabitor. The research on the inhibition effect between complexes and dipeptidyl peptidase was studied by DPP-IV screening model. It provides a theoretical base forscreening high effective, selectivity, low toxicity hypoglycemic drugs. Eight metal complexes were synthesized with salicylaldehyde and o-phenylene diamine as ligands. The compounds were characterized by the X-ray diffraction, infrared spectroscopy, fluorescence spectroscopy and other physical and chemical methods.On the other hand, the inhibitory activity of the eight mteal complexes to Human DPP-IV was studied by ELIASA. The experimental results show that the metal complexes1,3,4,6,7had inhibition effect to the DPP-IV. The IC50value of complex3was0.15umol/L, indicated that the complex have significant inhibitory effect. Moreover, the interaction of the eight metal complexes with DPP-IV was studied by molercular docking method and found the remarkable amino acid residues group with the inhibitor.Furthermore, the dissertation also discussed the antibacterial activity of seven metal complexes against MRSA. The experimental results show that complex1and complex2showed significant sensitive against Funguese in the screening test, complex1also showed sensitive against Escherichia coli and complex1and complex4showed sensitive against Staphylococcus aureus. Amazingly, complex1indicated significantly inhibitory effect on Escherichia colibetter than penicillin and rifampin in the susceptibility test. The complex1and complex2showed antibacterial activity against Staphylococcus aureus better than fluconazole.