Synthesis And Biological Evaluation Of Schiff Base Metal Complexes With N,O-bidentate Ligands As Urease Inhibitors

Schiff base ligands derived from the condensation of aromatic aldehydes is an importantclass of biological ligands. These Schiff base compounds can be used as bidentate N,O–andtridentate N,O,O–donor chelating ligands to synthesize many metal complexes with variousstructures and special properties. Schiff base metal complexes have been researched inchemistry, biology and materials science. For example, some Schiff base metal complexespossessing a clear anti-TB, anti-cancer, antibacterial and other pharmacological effects havebeen reported. Over the years, the study of such complexes as biological, pharmaceuticalchemistry and inorganic chemistry is a hot spot. In order to study and explore Schiff basemetal complexes with potent urease inhibition activity, a series of Schiff base ligands derivedfrom the condensation of aromatic aldehydes and metal complexes of Schiff bases asbidentate N,O–donor chelating ligands have been synthesized and characterized as the ureaseinhibitors.Due to 2-hydroxy-1-naphthaldehyde unique chemical properties such as structural strongconjugation and the large steric smaller naphthalene, a series of Schiff base ligands stronglycoordinating to metal ions have been synthesized in this paper, which are derived from thecondensation of 2-hydroxy-1-naphthaldehyde with primary amines. Many metal complexes ofSchiff bases as bidentate N,O–donor chelating ligands have been synthesized in this paper too.Among such Schiff base metal complexes, fifteen metal complexes were choosed andcharacterized. These metal complexes as the urease inhibitors were studied. Their biologicalactivities against the jack been urease were tested. The binding models of these Schiff basemetal complexes with jack bean urease were simulated using the Dock 4.2 program tovalidate their structure activity relationships. This may provide theoretical guidance for smallmolecule 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 suchcomplexes 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 sitewere modeled via software AUTODOCK 4.2 program.