Résumé
Objective:To synthesize substituted pyridine propynyl carbamates and to test their antimicrobial activities. Methods: Eight novel compounds were designed and synthesized. Antimicrobial tests in vitro were carried out with 8 common mildews (Aspergullus niger, Aspergillus flavus, Aspergillus versicolor, Trichoderma viride, Paecilomium varioti Bainier, Chaetomium globsum, Penicillium citrinum, Cladochytrium clodospoium) and 5 bacteria (Escherichia coli, Pseudomonas fluorescens, Bacillus fluorescens, Bacillus megatherium). Results: All compounds synthesized showed antimicrobial activity, especially the compound 1f, whose activity was more potent than that of compound 3-iodo-2-propynyl-butyl-carbamate (IPBC). Conclusion: Compound 1f is worth further studying and exploration.
Résumé
Objective:To synthesize disubstituted pyridine and I-substituted propynyl carbamates and study their antimicrobial activities, searching for more potent and less toxic antimicrobial agents.Methods: The title compounds were synthesized through the process of electrophilic and nucleophilic substitution. Antimicrobial test in vitro was determined with 13 kinds of common mildews and bacteria(Aspergullus niger, aspergillus flavus, Aspergillus versicolor,Trichoderma viride, Paecilomium varioti Bainier, Chaetomium globsum, Penicillium citrinum, Cladochytrium clodospoium, Escherichia colo, Staphylococcus aureus, Pseudomonas fluorescens Bacillus fluorescens, and Bacillus megatherium). The chemical structures of all compounds were determined by IR, 1 HNMR and elementary analysis.Results: Seven disubstituted pyridine and I-substituted propynyl carbamates obtained were firstly reported. All compounds showed antimicrobial activity, especially compound 3e, who had more potent activity compared with the that of 3-iodo-2-propynyl-butyl- carbamate (IPBC). MIC of the compound 3e was between 2?10 -6 g/ml to 30?10 -6 g/ml . Conclusion: Compound 3e has the best antimicrobial activity and should be futher studied.