Bioorg Med Chem Lett 2016 10 7;26(20):4925-4929. Epub 2016 Sep 7.
School of Life Sciences, Shandong University of Technology, Zibo 255000, PR China; State Key Laboratory of Pharmaceutical Biotechnology, Nanjing University, Nanjing 210093, PR China.
Three mononuclear Cu(II) complexes Cu(HL)Cl (1), Cu(HL)Cl (2), and Cu(L)SCN (3) have been synthesized based on chelating hydrazone ligands HL, HL, and HL, respectively. These new compounds gave satisfactory IR-spectroscopic data and were further characterized by elemental and X-ray diffraction analyses. Their urease inhibitory evaluation was tested in vitro against jack bean urease. The results showed that the inhibitory activities of the copper complexes are all superior to the positive reference. Enzyme kinetics studies were undertaken to estimate the inhibition mechanism of the copper complexes. Molecular docking simulations have been performed to rationalize their binding models. In addition, their interactions with serum albumin were also studied.