Synthesis and antimicrobial evaluation of L-phenylalanine-derived C5-substituted rhodanine and chalcone derivatives containing thiobarbituric acid or 2-thioxo-4-thiazolidinone
| Autor: | Li-Jun Yu, Xin Jin, Chang-Ji Zheng, Yin-Jing Li, Hu-Ri Piao, Yan Wu, Ming-Xia Song, Liang-Peng Sun |
|---|---|
| Rok vydání: | 2012 |
| Předmět: |
Chalcone
Staphylococcus aureus Rhodanine Stereochemistry Thiobarbituric acid Phenylalanine Microbial Sensitivity Tests medicine.disease_cause Minimum inhibitory concentration chemistry.chemical_compound Structure-Activity Relationship Drug Discovery medicine Pharmacology Dose-Response Relationship Drug Molecular Structure Organic Chemistry General Medicine Antimicrobial Thiobarbiturates Anti-Bacterial Agents chemistry Thiazolidines Antibacterial activity Nuclear chemistry |
| Zdroj: | European journal of medicinal chemistry. 56 |
| ISSN: | 1768-3254 |
| Popis: | Four novel series of compounds, including the l -phenylalanine-derived C5-substituted rhodanine (6a–q, 7a–j) and chalcone derivatives containing thiobarbituric acid or 2-thioxo-4-thiazolidinone (9a–e, 11a–e) have been designed, synthesized, characterized, and evaluated for their antibacterial activity. Some of these compounds showed significant antibacterial activity against Gram-positive bacterias, especially against the strains of multidrug-resistant clinical isolates, among which compounds 6c–e, 6g, 6i, 6j and 6q exhibiting high levels of antimicrobial activity against Staphylococcus aureus RN4220 with minimum inhibitory concentration (MIC) values of 2 μg/mL. Compound 6q showed the most potent activity of all of the compounds against all of the test multidrug-resistant clinical isolates tested. Unfortunately, however, none of the compounds were active against Gram-negative bacteria at 64 μg/mL. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
Full Text from ScienceDirect