Identification of novel aminopiperidine derivatives for antibacterial activity against Gram-positive bacteria.
Bioorg Med Chem Lett
; 26(13): 3148-3152, 2016 07 01.
Article
en En
| MEDLINE
| ID: mdl-27173797
ABSTRACT
We have previously reported amidopiperidine derivatives as a novel peptide deformylase (PDF) inhibitor and evaluated its antibacterial activity against Gram-positive bacteria, but poor pharmacokinetic profiles have resulted in low efficacy in in vivo mouse models. In order to overcome these weaknesses, we newly synthesized aminopiperidine derivatives with remarkable antimicrobial properties and oral bioavailability, and also identified their in vivo efficacy against methicillin-resistant Staphylococcus aureus (MRSA), vancomycin-resistant Enterococcus (VRE) and penicillin-resistant Streptococcus pneumoniae (PRSP).
Palabras clave
Texto completo:
1
Bases de datos:
MEDLINE
Asunto principal:
Piperidinas
/
Inhibidores Enzimáticos
/
Bacterias Grampositivas
/
Antibacterianos
Tipo de estudio:
Diagnostic_studies
Límite:
Animals
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2016
Tipo del documento:
Article