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Arch Pharm (Weinheim) ; 357(8): e2400047, 2024 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-38687910

RESUMEN

The emergence and global spread of methicillin-resistant Staphylococcus aureus (MRSA) pose a serious threat to public health, underscoring the urgent need for novel antibacterial interventions. Here, we screened 18 newly synthesized N,N'-diarylurea derivatives to identify compounds with activity against MRSA. Our investigations led to the discovery of a small molecule, SCB-24, which exhibited promising antimicrobial activity against MRSA USA300. Notably, SCB-24 demonstrated high activity even in the presence of 10% fetal bovine serum and showed excellent selectivity for bacterial over mammalian cells. SCB-24 also showed potent activity against various MRSA strains, including those resistant to second- and third-line antibiotics. Importantly, the efficacy of SCB-24 was inferior to that of vancomycin in MRSA-infected Galleria mellonella larvae. Overall, our findings suggest that SCB-24 has great potential as a new therapeutic for multidrug-resistant S. aureus infections.


Asunto(s)
Antibacterianos , Staphylococcus aureus Resistente a Meticilina , Pruebas de Sensibilidad Microbiana , Urea , Staphylococcus aureus Resistente a Meticilina/efectos de los fármacos , Antibacterianos/farmacología , Antibacterianos/síntesis química , Antibacterianos/química , Animales , Relación Estructura-Actividad , Urea/farmacología , Urea/química , Urea/análogos & derivados , Humanos , Larva/efectos de los fármacos , Estructura Molecular , Farmacorresistencia Bacteriana Múltiple/efectos de los fármacos , Mariposas Nocturnas/efectos de los fármacos , Mariposas Nocturnas/microbiología , Descubrimiento de Drogas , Infecciones Estafilocócicas/tratamiento farmacológico , Infecciones Estafilocócicas/microbiología , Relación Dosis-Respuesta a Droga
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