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Eur J Med Chem ; 70: 49-58, 2013.
Article in English | MEDLINE | ID: mdl-24140916

ABSTRACT

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 coli. Compound 5e exhibited highest anti-tubercular activity (0.46 µg/mL) close to that of standard Isoniazid (0.40 µg/mL). Equal antifungal activity (1.56 µg/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 µg/mL) and MRSA (MIC 0.78-1.56 µg/mL). All compounds were tested for mammalian cell toxicity using VERO cell line and were found to be non-toxic.


Subject(s)
Antibiotics, Antitubercular/pharmacology , Antifungal Agents/pharmacology , Oxadiazoles/pharmacology , Pyrroles/chemistry , Animals , Antibiotics, Antitubercular/chemical synthesis , Antibiotics, Antitubercular/chemistry , Antifungal Agents/chemical synthesis , Antifungal Agents/chemistry , Bacillus subtilis/drug effects , Candida albicans/drug effects , Chlorocebus aethiops , Dose-Response Relationship, Drug , Escherichia coli/drug effects , Microbial Sensitivity Tests , Molecular Structure , Mycobacterium tuberculosis/drug effects , Oxadiazoles/chemical synthesis , Oxadiazoles/chemistry , Staphylococcus aureus/drug effects , Structure-Activity Relationship , Vero Cells
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