Isocyanides in med chem: A scaffold hopping approach for the identification of novel 4-isocyanophenylamides as potent antibacterial agents against methicillin-resistant Staphylococcusaureus.
Eur J Med Chem
; 246: 114950, 2023 Jan 15.
Article
em En
| MEDLINE
| ID: mdl-36462437
ABSTRACT
We describe the rational use of the neglected isocyano moiety as pharmacophoric group for the design of novel 4-isocyanophenylamides as antibacterial agents. This class of novel compounds showed to be highly effective against methicillin resistant Staphylococcus aureus strains. In particular, from an extensive screening, we identified compound 42 as lead compound. It has shown a potent antimicrobial activity, an additive effect with most antibiotics currently in use, the ability not to induce the formation of resistant strains after ten passages, and the ability to block the biofilm formation. A nontoxic profile on mammalian cells and a proper metabolic stability on human liver microsome complete the picture of this new weapon against methicillin resistant Staphylococcus aureus infections.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Staphylococcus aureus Resistente à Meticilina
/
Antibacterianos
Tipo de estudo:
Diagnostic_studies
Limite:
Animals
/
Humans
Idioma:
En
Ano de publicação:
2023
Tipo de documento:
Article