期刊
JOURNAL OF THE SERBIAN CHEMICAL SOCIETY
卷 77, 期 1, 页码 9-16出版社
SERBIAN CHEMICAL SOC
DOI: 10.2298/JSC110123155M
关键词
1,3,4-oxadiazoles; antimicrobial activity; isoniazid; Mannich bases; lipophilicity
Structural modifications of the front line antitubercular drug isoniazid provide lipophilic adaptations of the drug in which the hydrazide moiety of isoniazid is replaced by 1,3,4-oxadiazole heterocycles to eliminate in vivo acetylation by arylamine N-acetyltransferase, which results in the formation of inactive acetylated drug. In the present study, a series of sixteen oxadiazole derivatives were synthesized and characterized by IR, H-1-NMR, C-13-NMR and mass spectral studies. All the synthesized compounds were evaluated for their antimicrobial activity by broth dilution method against two Gram-positive bacterial strains (Bacillus subtilis and Staphylococcus aureus), two Gram-negative bacterial strains (Pseudomonas aeruginosa and Escherichia coli) and two fungal strains (Candida albicans and Aspergillus niger). The minimum inhibitory concentrations of the compounds were in the range of 1.56-50 mu g ml(-1) against the bacterial and fungal strains. The results revealed that all the synthesized compounds have a significant biological activity against the tested microorganisms. Among the synthesized derivatives 4g, 4h, 4m and 4p were found to be the most effective antimicrobial compounds.
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