Reseach On Syntheses And Biological Ctivity Of Chalcones-imidazole Erivatives

Chalcone moieties are common substructures in numerous natural productsbelonging to the flavonoid family. Chalcone derivatives are very versatile asphysiologically active compounds and substrates for the evaluation of variousorganic syntheses. These compounds have been reported to possess severalbiological activities， such as cytotoxic， antimalarial， antileishmanial， anti-inflammatory， anti-HIV， antifungal and as tyrosine kinase inhibitors. Havingsuch varied pharmacological activities，these molecules have attracted medicinalchemists and therefore several strategies have been developed to synthesizethem.In recent years, heterocyclic compounds played an important roleincreasingly in research and development of new drugs. Among five memberedheterocycles, imidazole represents was a class of compounds of great importancein biological chemistry. Imidazole and its derivatives have great significance dueto their important roles in biological systems, particularly in enzymes, as protondonors and/or acceptors, coordination system ligands and the base of charge–transfer processes. Unlike pyrrole (a proton donor) and pyridine (a protonacceptor),1H-imidazole has both proton donor and acceptor properties.Imidazole functionalities have been used for complex reactions with differentmolecular components such as carboxylic acids to obtain liquid crystallineassemblies. The imidazole nucleus appears in a number of naturally occurringproducts like the amino acids histidine and purines, which comprise many of themost important bases in nucleic acids. Imidazole derivatives are gainingsynthetic interest in recent years due to their broad spectrum of biologicalactivities，for instance，a broad spectrum of pharmacological activities such asanticonvulsant, anti-Parkinson, antiinflammatory，analgesic，antibacterial andantifungal.For all of reasons， A novel of12-membered chalcone-imidazole derivativeshave been synthesized and characterized by IR，1HNMR，13CNMR and elementalanalysis，the analysis results conformed to the structures that we expected. Substituted acetophenones and benzaldehydes were condensed using theClaisen–Schmidt base catalyzed aldol condensation. Methyl on the aromatic ringof Chalcones was brominated by NBS，and then the resulting mixture reactedwith imidazole to get target compound. Several chalcones showed good activityin vitro antibacterial activity against bacterial, for example (E)-1-(4-((1H-imidazol-1-yl)methyl)phenyl)-3-(4-fluorophenyl)prop-2-en-1-one,(E)-1-(4-((1H-imidazol-1-yl)methyl)phenyl)-3-(3-nitrophenyl)prop-2-en-1-one,(E)-1-ferroceneylprop-3-(4-((1H-imidazol-1-yl)methyl)phenyl)-2-en-1-one, and (E)-1-(4-fluorophenyl)phenylprop-3-(4-((1H-imidazol-1-yl)methyl)phenyl)-2-en-1-one.The result showed that these are potential antibacterial compounds. Meanwhile,we have been studied and detemined the optimal synthesized conditiongs ofchalcone-imdazole derivatives.