AI Article Synopsis
- Antimicrobial resistance poses a significant public health threat, driving the need for new antimicrobial agents targeting resistant bacteria.
- Research presents cationic chlorpromazine peptide conjugates, particularly the compound CPWL, which effectively fights multidrug-resistant S. aureus without harming human cells.
- Molecular docking and MD simulation studies demonstrate CPWL's strong binding affinity to saFabI, marking it as a potential candidate for developing inhibitors to combat severe staphylococcal infections.
Article Abstract
Antimicrobial resistance is a serious public health risk. Its severity is fueled on an unprecedented scale, necessitating the demand for novel antimicrobial scaffolds aimed at novel targets. Herein, we present cationic chlorpromazine peptide conjugates that are rationally intended to targetmultidrug-resistant (MDR) bacteria. The most potent compound, CPWL, of all the conjugates evaluated, showed promising antibacterial activity against clinical, MDR S. aureus, with no cytotoxicity. The molecular docking experiments confirmed that CPWL possessed a very high affinity for S. aureus enoyl reductase (saFabI). Furthermore, CPWL antibacterial action against saFabI was further corroborated by MD simulation studies. Thus, our findings highlight cationic chlorpromazine as a promising scaffold for the development of saFabI inhibitors to target severe staphylococcal infections.
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| http://dx.doi.org/10.1002/asia.202300169 | DOI Listing |
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