Preparation And Antibacterial Activity Of Quinolone Alkynyl Derivatives-polyolefin Film Materials

Objective A series of novel quinolone alkynyl derivatives were prepared by using organoalkyne ligands,triazole ligands and metallic silver to modify norfloxacin and ciprofloxacin,and the antibacterial activity of the derivatives was tested.The influence of the modification of ligands and metallic silver on the antibacterial activity of the raw material drugs was studied.A series of antibacterial polymer polystyrene macromolecule films were prepared using the derivatives with better antibacterial activity as antibacterial agents.Provides new structural models and basic data for the research and development of clinical antibacterial drugs and antibacterial polymer materials.Methods In the conventional organic phase,a series of quinolone alkynyl derivatives are obtained through a nucleophilic substitution reaction,a nitrogen heterocyclic reaction,and a coordination reaction.The new quinolone derivatives were characterized by X-ray single crystal diffraction,NMR,IR,MS and elemental analysis.The antibacterial activity of the quinolone derivatives were studied in vitro using Disk diffusion test and powder antibacterial experiments.The quinolone derivatives with good antibacterial effect were selected as antibacterial agent to prepare polystyrene films with antibacterial activity.Finally,the antibacterial activity of the antibacterial films were studied using the antibacterial property test of the films.Results Two new quinolone alkynyl derivatives,four quinolone alkynyl triazole derivatives and two silver quinolone alkyne complexes were successfully synthesized.Two new quinolone alkynyl derivatives,four quinolone alkynyl triazole derivatives and two silver quinolone alkyne complexes were successfully synthesized.Four kinds of polystyrene macromolecule antibacterial films were prepared using compounds 1a,2a,1d,and 2d as antibacterial agents.The activity test analysis showed that the bactericidal performance of the alkynyl derivatives were slightly lower than that of the raw material drugs;the bactericidal performance of the triazole derivatives were greatly reduced;the bactericidal performance of the silver complexes were greatly improved.At the same time,four antibacterial films can inhibit the growth of S.aureus and E.coli.Conclusion In the design and synthesis of antibacterial agents,the introduction of alkynyl and triazole nucleus will reduce the antibacterial activity in different degrees,but the introduction of silver ions in alkynyl derivatives will lead to an increase in the antibacterial activity of the compound due to the synergistic antibacterial effect.The four antibacterial films have a good inhibitory effect on the pathogenic bacteria selected for the experiment.The above derivatives and the preparation of antibacterial polymers can provide some basic experimental data for the future transformation of quinolones,and can also provide new ideas and new antibacterial materials for the preparation of antibacterial polymer materials.