期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 70, 期 -, 页码 49-58出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2013.09.039
关键词
4-Nitropyrrole; 1,3,4-Oxadiazole; Antimicrobial agent; Antifungal agent; Anti-tubercular agent
We report synthesis and antimicrobial evaluation of 42 novel 4-nitropyrrole-based 1,3,4-oxadiazoles. The synthesized molecules were evaluated for anti-bacterial, anti-fungal and anti-tubercular activities. Promisingly, most of the compounds showed equal or more potency than standard ciprofloxacin against Staphylococcus aureus, Bacillus subtilis and Escherichia coll. Compound 5e exhibited highest antitubercular activity (0.46 mu g/mL) close to that of standard Isoniazid (0.40 mu g/mL). Equal antifungal activity (1.56 mu g/mL) compared to standard Amphotericin-B was shown by most of the compounds. All the N-methylated compounds showed more potent to equal activity against MSSA (MIC 0.39-1.56 mu g/mL) and MRSA (MIC 0.78-1.56 mu g/mL). All compounds were tested for mammalian cell toxicity using VERO cell line and were found to be non-toxic. (C) 2013 Elsevier Masson SAS. All rights reserved.
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