Design, synthesis, and antibacterial evaluation of PFK-158 derivatives as potent agents against drug-resistant bacteria
| Autor: | Guoning Zhang, Juxian Wang, You-Wen Zhang, Xue-Mei Li, Niu Weiping, Fan Zhang, Mei Zhu, Minghua Wang, Wang Wei, Shang-Jiu Hu |
|---|---|
| Rok vydání: | 2020 |
| Předmět: |
Drug
Staphylococcus aureus medicine.drug_class Pyridines media_common.quotation_subject Polymyxin Clinical Biochemistry Pharmaceutical Science Antibacterial effect Microbial Sensitivity Tests 01 natural sciences Biochemistry Microbiology Structure-Activity Relationship Antibiotic resistance Levofloxacin Staphylococcus epidermidis Drug Discovery medicine Molecular Biology media_common biology Dose-Response Relationship Drug Molecular Structure 010405 organic chemistry Chemistry Organic Chemistry Vancomycin Resistance biology.organism_classification 0104 chemical sciences Anti-Bacterial Agents 010404 medicinal & biomolecular chemistry Drug Design Quinolines Molecular Medicine Methicillin Resistance Bacteria Enterococcus Phosphofructokinase medicine.drug |
| Zdroj: | Bioorganicmedicinal chemistry letters. 41 |
| ISSN: | 1464-3405 |
| Popis: | Infections caused by antibiotic resistant bacteria are a major health concern throughout the world. It is well known that PFK-158 can enhance the antibacterial effect of polymyxin, but its own anti-bactericidal effect is rarely discussed. In order to investigate the anti-bactericidal effect of PFK-158 and its derivatives, PFK-158 and 35 derivatives were designed, synthesized, and evaluated for their antibacterial activities. Compounds A1, A3, A14, A15 and B6 exhibited potent antibacterial effect against both clinical drug sensitive and resistant Gram-positive bacteria, and they are 2-8 folds more potent than levofloxacin against Methicillin-resistant staphylococcus epidermidis (MRSE). A significant synergistic effect of these compounds and polymyxin against drug-resistant Gram-negative bacteria, which is similar to PFK-158 was also observed. The result can provided a new and broader prospect for the development of new medicine against drug-resistant bacteria. |
| Databáze: | OpenAIRE |
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