Synthesis, structure and urease inhibition studies of Schiff base copper(II) complexes with planar four-coordinate copper(II) centers

J Inorg Biochem. 2013 Oct:127:82-9. doi: 10.1016/j.jinorgbio.2013.07.036. Epub 2013 Aug 2.

Abstract

Seven new Schiff base copper(II) complexes with planar four-coordinate copper(II) centers have been synthesized and structurally characterized. The solid state structures of complexes 1, 3, 4, 5, 6 and 7 present a square-planar coordination geometry at the metal centers while complex 2 shows a slightly distorted square-planar geometry. Density functional theory calculations have been performed to evaluate the electronic structure of copper(II) complex 7. Inhibition of jack bean urease by copper(II) complexes 1-7 have also been investigated, and potent inhibitory activities with IC50 range of 2.60-17.00μM have been observed for these mononuclear copper(II) complexes. A docking analysis using a DOCK program was conducted to explain the urease inhibitory activity of the copper(II) complexes and the structure-activity relationships were further discussed.

Keywords: Copper(II) complexes; Density functional calculations; Molecular docking; Urease inhibitors; X-ray structures.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Coordination Complexes / chemical synthesis*
  • Coordination Complexes / chemistry
  • Coordination Complexes / pharmacology
  • Copper / chemistry*
  • Crystallography, X-Ray
  • Enzyme Activation / drug effects
  • Enzyme Inhibitors / chemical synthesis
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / pharmacology
  • Models, Molecular
  • Quantum Theory*
  • Schiff Bases / chemistry*
  • Structure-Activity Relationship
  • Urease / antagonists & inhibitors*

Substances

  • Coordination Complexes
  • Enzyme Inhibitors
  • Schiff Bases
  • Copper
  • Urease