Development of a Dual-Acting Antibacterial Agent (TNP-2092) for the Treatment of Persistent Bacterial Infections
| Autor: | Zhenkun Ma, Anthony Simon Lynch |
|---|---|
| Rok vydání: | 2016 |
| Předmět: |
0301 basic medicine
Drug Staphylococcus aureus medicine.drug_class media_common.quotation_subject 030106 microbiology Antibiotics Rifamycins Microbial Sensitivity Tests medicine.disease_cause Microbiology 03 medical and health sciences Structure-Activity Relationship Drug Discovery polycyclic compounds medicine media_common Antibacterial agent biology Dose-Response Relationship Drug Molecular Structure Drug candidate Rifamycin Bacterial Infections biology.organism_classification Anti-Bacterial Agents 030104 developmental biology Molecular Medicine Bacteria |
| Zdroj: | Journal of medicinal chemistry. 59(14) |
| ISSN: | 1520-4804 |
| Popis: | The clinical management of prosthetic joint infections and other persistent bacterial infections represents a major unmet medical need. The rifamycins are one of the most potent antibiotic classes against persistent bacterial infections, but bacteria can develop resistance to rifamycins rapidly and the clinical utility of the rifamycin class is typically limited to antibiotic combinations to minimize the development of resistance. To develop a better therapy against persistent bacterial infections, a series of rifamycin based bifunctional molecules were designed, synthesized, and evaluated with the goal to identify a dual-acting drug that maintains the potent activity of rifamycins against persistent pathogens and at the same time minimize the development of rifamycin resistance. TNP-2092 was identified as a drug candidate and is currently in an early stage of clinical development for the treatment of prosthetic joint infections. |
| Databáze: | OpenAIRE |
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