Evaluation of the monoamine oxidases inhibitory activity of a small series of 5-(azole)methyl oxazolidinones
| Autor: | Leyla H. Sharaf, Roselyn Jennifer D’silva, Ludmil Benov, Oludotun A. Phillips, Edet E. Udo |
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| Rok vydání: | 2015 |
| Předmět: |
chemistry.chemical_classification
Monoamine Oxidase Inhibitors biology Stereochemistry Structural similarity Gram-positive bacteria Pharmaceutical Science Pathogenic bacteria medicine.disease_cause biology.organism_classification Anti-Bacterial Agents Toloxatone chemistry.chemical_compound Monoamine neurotransmitter chemistry Linezolid medicine Azole Antibacterial activity Monoamine Oxidase Oxazolidinones medicine.drug |
| Zdroj: | European Journal of Pharmaceutical Sciences. 71:56-61 |
| ISSN: | 0928-0987 |
| DOI: | 10.1016/j.ejps.2015.02.006 |
| Popis: | Oxazolidinone class of compounds continue to generate interest as promising agents effective against sensitive and resistant Gram-positive pathogenic bacteria strains. Recent focus is to develop new potent derivatives with improved broad-spectrum activity and safety profile superior to linezolid. An important toxicity issue for this class of compounds arises from the structural similarity with toloxatone, a known MAO inhibitor. Herein, we report the evaluation of a small series of 5-(1H-1,2,3-triazolyl)-, 5-(4-methyl-1H-1,2,3-triazolyl)-, 5-(5-methyl-1H-1,2,3-triazolyl)- and 5-imidazolyl-methyl oxazolidinone analogs with and without antibacterial activity for their effects as inhibitors of monoamine-A and -B (MAO-A and -B) oxidases. Substitutions at the oxazolidinone C-5 position significantly affected antibacterial activity and MAO inhibition. The N-substituted-glycinyl 1H-1,2,3-triazolyl methyl oxazolidinones with potent antibacterial activity demonstrated only weak to moderate affinity for MAO-A and -B, supporting further investigation for this group of compounds. |
| Databáze: | OpenAIRE |
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