The synthesis of phenylalanine-derived C5-substituted rhodanines and their activity against selected methicillin-resistant Staphylococcus aureus (MRSA) strains
| Autor: | Diane Hardej, Satyakam Singh, Shridhar S. Kulkarni, Tanaji T. Talele, Nikhil Khadtare, Charles R. Ashby |
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| Rok vydání: | 2010 |
| Předmět: |
Methicillin-Resistant Staphylococcus aureus
Meticillin Rhodanine medicine.drug_class Stereochemistry Phenylalanine Antibiotics Microbial Sensitivity Tests medicine.disease_cause Microbiology Structure-Activity Relationship Drug Discovery medicine Antibacterial agent Pharmacology Dose-Response Relationship Drug Molecular Structure Chemistry Organic Chemistry Stereoisomerism General Medicine Methicillin-resistant Staphylococcus aureus Anti-Bacterial Agents Penicillin Ciprofloxacin Staphylococcus aureus Vancomycin medicine.drug |
| Zdroj: | European Journal of Medicinal Chemistry. 45:5827-5832 |
| ISSN: | 0223-5234 |
| DOI: | 10.1016/j.ejmech.2010.09.045 |
| Popis: | A series of rhodanine compounds containing various substituents at the N3- and C5-positions were synthesized and their in vitro activity against a panel of clinically relevant MRSA strains was determined. The anti-MRSA activity of compounds 21 (MIC = 3.9 μg/mL, MBC = 7.8 μg/mL) and 22 (MIC = 1.95 μg/mL, MBC = 7.8 μg/mL) was significantly greater than that of the lead compounds, 1–3 and reference antibiotics penicillin G (MIC = 31.25 μg/mL) and ciprofloxacin (MIC = 7.8 μg/mL) and comparable to that of vancomycin (MIC = 0.97 μg/mL). Compounds 21 and 22 were found to be bactericidal at only 2–4-fold higher than their MIC concentrations. In addition, their MIC values remained unchanged in the presence or absence of 10% serum. Overall, the results suggest that compounds 21 and 22 may be of potential use in the treatment of MRSA infections. |
| Databáze: | OpenAIRE |
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