Structure-Antibacterial Activity Relationships of N-Substituted-(d-/l-Alaninyl) 1H-1,2,3-Triazolylmethyl Oxazolidinones
| Autor: | Edet E. Udo, Roselyn Jennifer D’silva, Oludotun A. Phillips |
|---|---|
| Jazyk: | angličtina |
| Rok vydání: | 2018 |
| Předmět: |
life_sciences_other
0301 basic medicine SARs Stereochemistry Substituent Pharmaceutical Science lcsh:RS1-441 linezolid alaninyl-oxazolidinone medicine.disease_cause Enterococcus faecalis Moraxella catarrhalis lcsh:Pharmacy and materia medica 03 medical and health sciences chemistry.chemical_compound Antibiotic resistance Staphylococcus epidermidis medicine biology triazolyl-oxazolidinone biology.organism_classification antibacterial 030104 developmental biology chemistry Staphylococcus aureus Linezolid Antibacterial activity |
| Zdroj: | Scientia Pharmaceutica, Vol 86, Iss 4, p 42 (2018) Scientia Pharmaceutica Volume 86 Issue 4 |
| ISSN: | 2218-0532 |
| Popis: | Bacterial resistance towards the existing class of antibacterial drugs continues to increase, posing a significant threat to the clinical usefulness of these drugs. These increasing and alarming rates of antibacterial resistance development and the decline in the number of new antibacterial drugs&rsquo approval continue to serve as a major impetus for research into the discovery and development of new antibacterial agents. We synthesized a series of d-/l-alaninyl substituted triazolyl oxazolidinone derivatives and evaluated their antibacterial activity against selected standard Gram-positive and Gram-negative bacterial strains. Overall, the compounds showed moderate to strong antibacterial activity. Compounds 9d and 10d (d- and l-alaninyl derivatives bearing the 3,5-dinitrobenzoyl substituent), 10e (l-alaninyl derivative bearing the 5-nitrofurancarbonyl group) and 9f and 10f (d- and l-alaninyl derivatives bearing the 5-nitrothiophene carbonyl moiety) demonstrated antibacterial activity (MIC: 2 µ g/mL) against Staphylococcus aureus, Staphylococcus epidermidis, Enterococcus faecalis and Moraxella catarrhalis standard bacterial strains. No significant differences were noticeable between the antibacterial activity of the d- and l-alaninyl derivatives as a result of the stereochemistry of the compounds. |
| Databáze: | OpenAIRE |
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