The Synthesis And Antibacterial Activity Of Two Types Of Polyhalogen Substituted Cyanoarylamine Compounds

Natural organic halide and cyanide widely exist in nature,and play a variety of important physiological role.Since the fluorine atoms have electronic effects,analog effect,penetration effect and obstruction effects,the fluorine-containing compound in the living body has an important function.Drug susceptibility testing is designed to understand the sensitivity of pathogenic microorganism to drug,to guide the rational use of antimicrobial agents in clinical microbiobgy tests.We designed and synthesized two types of polyhalogenated cyanoaromatic amines compounds and researched the antibacterial activity on basis of polyhaki isophthabnitriles possessing drug activity.The first chapter introduces the application in medicine of organic halides,organic cyanide and aromatic amines and the methods of antimicrobial activity tests.In the second chapter,we synthesis obtain high yields of novel chiral polyhatogenated aromatic amines by one step of the readily available materials polyhafo isopht halo nitriles with a chiral amino acid under alkaline conditions.New synthesized 26 compounds pass the test of antimicrobial activity,most of the compounds showed antibacterial activity oppose gram-positive bacterial.The third chapter,19 halogenated benzylanine compounds were obtained through one-step chemical roUte which polyhalo isophthalonitrilesre acted with benzyl arnine compounds in d ioxane solvent.A fter the test of antimicrobial activity.the activity of individual compounds were sIperior to marketable drug norfloxiacin.Five derivatives,5a(MBC[SA]=4.6 ?g/mL,MBC[BC]=5.2 ?g/mL);5b(MBC[SA]=5.2 ?g/mL,MBC[BC]=3.3 ?g/mL);5p(MBC[SA]=5.2 ?g/mL,MBC[BC]-5.2?g/mL);5q(MBC[SA]=2.6 ?g/mL)were identified good activity against gram-positive bacterial;Five derivatives,5b(MBC=10.4 ?g/mL);5d(MB=13.0?g/mL);5p(MBC=20.8 ?g/mL)have better activity against Candida albicans.All the structure of 45 target compounds was identified by 1H NMR,13C NMR,IR and MS spectral.