Preparations, characterization, and biological features of mononuclear Cu(II) complexes based on hydrazone ligands.

Authors :: Qin J
Zhao SS
Liu YP
Man ZW
Wang P
Wang LN
Xu Y
Zhu HL
Source :: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2016 Oct 15; Vol. 26 (20), pp. 4925-4929. Date of Electronic Publication: 2016 Sep 07.
Publication Year :: 2016
Abstract: Three mononuclear Cu(II) complexes Cu(HL <superscript>1</superscript> )Cl <subscript>2</subscript> (1), Cu(HL <superscript>2</superscript> )Cl <subscript>2</subscript> (2), and Cu(L <superscript>3</superscript> )SCN (3) have been synthesized based on chelating hydrazone ligands HL <superscript>1</superscript> , HL <superscript>2</superscript> , and HL <superscript>3</superscript> , 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.<br /> (Copyright © 2016 Elsevier Ltd. All rights reserved.)

Subjects :: Enzyme Inhibitors pharmacology
Ligands
Molecular Docking Simulation
Spectrophotometry, Infrared
Urease antagonists & inhibitors
X-Ray Diffraction
Copper chemistry
Hydrazones chemistry

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