Study On Synthesis,characterization And Ptp1b Inhibitory Activity Of Vanadium Complexes With Small Molecules

Over the years,as people living standard rise,diabetes has become one of the common and high incidence of diseases,causing serious harm to humans,so far have not found effective therapeutic methods and means,so the prevention and treatment of diabetes have become the focus of scientific research.There are many factors that cause diabetes,two of the key factors are insulin secretion and insulin resistance.Scientific studies have shown that PTP1B(protein tyrosine phosphatase 1B)specific inhibitors are highly desirable as drugs for the treatment of diabetes caused by insulin resistance.Vanadium compounds have insulin-like activity,the inorganic vanadium compounds are highly active,but they are very toxic,and their lipid solubility is not good in the organism,which is bad for the absorption of human body.Therefore,the synthesis of vanadium organic complexes and the inhibitory activity of PTP1 B enzyme have become the focus of research.In this paper,four kinds of vanadium small molecule complexes were designed and synthesized on the basis of a large number of previous literatures,namely: acetylacetonate vanadyl complexes,vanadium hydroxylamido complexes,Schiff base vanadyl complexes and pyridine vanadyl complexes.The research results are divided into the following parts: 1.Schiff base vanadyl complexesAfter reading a large number of documents and the research results of the research group,two new Schiff base vanadyl complexes were designed and synthesized,namely 5-chlorosalicylaldehyde trichloropropylamine Schiff base vanadyl,5-nitro Salicylaldehyde 2-chloroethylamine Schiff base vanadyl.In addition,in the design of the synthetic o-vanillyl o-aminophenyl acid Schiff base-2,2-bipyridyl vanadyl complex,we did not obtain the target product Schiff base,and obtained a 2,2-bipyridyl vanadyl complex.A series of characterizations of the above complexes have been carried out: elemental analysis,infrared spectroscopy,analysis of the composition of the complexes;the structure and geometric configuration of the complexes have been determined by single crystal X-ray diffraction.2.Hydroxylamine vanadium complexesBased on previous work,two new hydroxylamine vanadium complexes have been synthesized: vanadium hydroxylamido complex with oxalic acid(sodium as an external ion)and 2-amino-5-methylphenyl hydroxylamine vanadyl.A series of characterizations of these two complexes have been carried out: elemental analysis,infrared spectroscopy,analysis of the composition of complexes,and the use of X-rays Single crystal diffraction determines the structure and geometry of the complex.3.Vanadium acetylacetonate complexesEight new oxyacetylacetonate complexes were synthesized by evaporation method using organic small molecule ligands with benzene ring and vanadium transition metal under heating and refluxing.Respectively2-amino-6-chlorobenzoic acid acetylacetone o-phenanthroline vanadium complex,2-amino-5-chlorobenzoic acid acetylacetone o-phenanthrene 2-amino-5-iodobenzoic acid acetylacetone o-phenanthroline vanadium complexes,2-amino-5-iodobenzoic acid acetylacetone o-phenanthroline vanadium complexes In complexes,3-amino-2,4,6-tribromobenzoic acid acetylacetone o-phenanthroline vanadium complex,2,5-difluorobenzoic acid acetylacetone o-phenanthroline vanadium complex,2,5-dichloro Benzoic acid acetylacetone o-phenanthroline vanadium complexe.These eight complexes were characterized by several basic representations.The composition and molecular structure of the complexes were studied by elemental analysis and IR spectra.The XThe crystal structure and crystal purity of the complex were studied by diffraction and X-ray powder diffraction.4.Performance test of complexesThe 13 complexes synthesized were subjected to the measurement of the partition coefficient(lipophile analysis of the complex)and the PTP1 B enzyme inhibition activity test.Fat-soluble analysis showed that the complexes were all fat-soluble,indicating that they possessed the prerequisite for being a potential drug.The results of the PTP1 B enzyme activity test showed that the hydroxylamine oxetamine oxalate and the 2,2-dipyridyl vanadyl complex all showed some insulin-like activity,so our future research focus can be on these two types of vanadium complexes;Although the other vanadium complexes do not exhibit activity,their test results can accumulate experimental data for us to better synthesize and study vanadium complexes with insulin-like activity and further enrich the bioinorganic chemistry content.