Heterocyclic acyl-phosphate bioisostere-based inhibitors of Staphylococcus aureus biotin protein ligase.
Bioorg Med Chem Lett
; 24(19): 4689-4693, 2014 Oct 01.
Article
em En
| MEDLINE
| ID: mdl-25193234
ABSTRACT
Inhibitors of Staphylococcus aureus biotin protein ligase (SaBPL) are generated by replacing the acyl phosphate group of biotinyl-5'-AMP with either a 1,2,3-triazole (see 5/10a/10b) or a 1,2,4-oxadiazole (see 7) bioisostere. Importantly, the inhibitors are inactive against the human BPL. The nature of the 5-substituent in the component benzoxazolone of the optimum 1,2,3-triazole series is critical to activity, where this group binds in the ATP binding pocket of the enzyme.
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Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Organofosfatos
/
Proteínas de Bactérias
/
Biotina
/
Inibidores Enzimáticos
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Compostos Heterocíclicos
/
Ligases
Limite:
Humans
Idioma:
En
Ano de publicação:
2014
Tipo de documento:
Article