Targeting multidrug resistant Staphylococcus aureus with cationic chlorpromazine-peptide conjugates.
Chem Asian J
; 18(10): e202300169, 2023 May 16.
Article
in En
| MEDLINE
| ID: mdl-37071585
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.
Key words
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Staphylococcal Infections
/
Methicillin-Resistant Staphylococcus aureus
Limits:
Humans
Language:
En
Journal:
Chem Asian J
Year:
2023
Document type:
Article
Affiliation country: