Synthesis And Antibacterial Activities Of 3-substitutedthiol-4-substituted Amino-5-substituted1,2,4-triazoles Compounds

According to the latest report of bioinformatics, o-hydroxy diphenyl ether compounds and compounds containing thiazole ring in the anti-fungal, anti-bacterial, anti-virus with biological activity, low toxicity, specificity and other features, including "o-hydroxy benzene Base "and" triazole rings "are the two classes of compounds specifically target molecules and the core of effective combination; addition, according to the principle of superposition of biologically active compounds, speculated that some anti-bacterial, anti-viral activity of azole compounds excellent, with " O-hydroxyphenyl "modification or replacement part of the structure, composition and target new compounds may have a stronger affinity.5-substituted-4-amino-3-mercapto-1,2,4-triazole, exist in the structure of two adjacent amino and thiol nucleophilic site of action, can be transformed into a number of new heterocyclic structures In particular with aromatic aldehydes to form amino triazole Schiff has a good coordination ability. Therefore, we created based on the principle of the drug, the use of biological activity of the superposition principle, drawing on previous studies by our group, different mechanisms of the active group and the triazole ring o-hydroxyphenyl reasonable to the same molecular assembly, in the 4-amino-3-mercapto-1,2,4-triazole parent structure introduced in the 5 o-hydroxyphenyl, 3-mercapto will choose a different substitution groups, 4-amino and aromatic aldehydes, to form a good coordination ability Triazole Schiff base, o-hydroxy benzene to Kiki through the introduction of group and 5 (substituted) substituted benzene ring the changes and have the ability to coordinate the formation of Schiff bases have excellent antibacterial activity to find new compounds, this Three series of 30 synthetic compounds, compounds were confirmed by 1H NMR, IR and characterized to confirm.Inhibition tests showed that a concentration of 0.01%, the three series of target compounds on Candida albicans, the inhibitory rate of E.coli up to 89% or more, with strong antibacterial activity; on the inhibition of Staphylococcus aureus rate 84% have some antibacterial activity, especially acetophenone, acetophenone lactam ring has NO₂, Cl, Br substituted compounds on Escherichia coli, Staphylococcus aureus, Candida albicans, and antibacterial activity reached 93⁹9%, is the great potential of the anti-fungal, anti-Gram-negative bacteria compounds.structure-activity relationship showed that the thiazole ring structure on antimicrobial activity of compounds much of Candida albicans, E.coli, antibacterial activity, the general performance of the triazole-Schiff base-reducing compounds> triazole-Schiff bases Triazole compounds-parallel ring compounds, three compounds, molecules, fragments of the bridge connecting the two aromatic compounds based on antimicrobial activity have important implications to-SCH₂CONH-based compounds for the bridge than the bridge-SCH₂CO-The antibacterial activity of compounds, but also higher than the class of parallel rings, indicating that the introduction of amide and carbonyl compounds can improve the antibacterial activity; phenyl substituents on the antibacterial activity of the compounds have important implications for the introduction of the benzene ring NO₂, Cl, Br compounds can improve the antibacterial activity.