Synthesis And Urease Inhibition Studies Of Schiff Base Copper(Ⅱ) Complexes With O,N,O/O,N,N-Tridentate Ligands

Schiff base ligands derived from the condensation of aromatic aldehydes is an important class of biological ligands. These Schiff base compounds can be used as bidentate N,O-and tridentate O,N,O/O,N,N-donor chelating ligands to synthesize many metal complexes with various structures and special properties. Schiff base metal complexes have been researched in chemistry, biology and materials science. For example, some Schiff base metal complexes possessing a clear anti-TB, anti-cancer, antibacterial and other pharmacological effects have been reported. Over the years, the study of such complexes as biological, pharmaceutical chemistry and inorganic chemistry is a hot spot. In order to study and explore Schiff base metal complexes with potent urease inhibition activity, a series of Schiff base ligands derived from the condensation of aromatic aldehydes and metal complexes of Schiff bases as tridentate O,N,O-donor chelating ligands have been synthesized and characterized as the urease inhibitors.A series of Schiff base ligands strongly coordinating to Cu(Ⅱ) ions have been synthesized are derived from the condensation of hydrazide, amino acids, piperidine with different aldehydes compounds. Many Cu(Ⅱ) complexes of Schiff bases as those tridentate O,N,O-donor chelating ligands have been synthesized in this paper. Among such Schiff base complexes, fifteen complexes1-15were choosed and characterized. These Cu(Ⅱ) complexes as the urease inhibitors were studied. Their biological activities against the jack been urease were tested. The binding models of these Schiff base metal complexes with jack bean urease were simulated using the Dock4.2program to validate their structure-activity relationships. This may provide theoretical guidance for small molecule urease inhibitors.The following is mainly researched work in this paper:1. A review of Schiff base metal complexes reported in literatures was did;2. More than forty new Schiff base complexes were synthesized and fifteen such complexes were further characterized;3. The activity of these Schiff base metal complexes against Jack been urease was tested. The structure-activity relationship was discussed;4. The binding modes of these Schiff base metal complexes in the enzyme active site were modeled via software AUTODOCK4.2program.