Benzimidazole analogs as WTA biosynthesis inhibitors targeting methicillin resistant Staphylococcus aureus.
Bioorg Med Chem Lett
; 26(19): 4743-4747, 2016 10 01.
Article
em En
| MEDLINE
| ID: mdl-27575474
ABSTRACT
A series of benzimidazole analogs have been synthesized to improve the profile of the previous lead compounds tarocin B and 1. The syntheses, structure-activity relationships, and selected biochemical data of these analogs are described. The optimization efforts allowed the identification of 21, a fluoro-substituted benzimidazole, exhibiting potent TarO inhibitory activity and typical profile for a wall teichoic acid (WTA) biosynthesis inhibitor. Compound 21 displayed a potent synergistic and bactericidal effect in combination with imipenem against diverse methicillin-resistant Staphylococci.
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Base de dados:
MEDLINE
Assunto principal:
Ácidos Teicoicos
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Benzimidazóis
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Staphylococcus aureus Resistente à Meticilina
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Antibacterianos
Limite:
Animals
Idioma:
En
Ano de publicação:
2016
Tipo de documento:
Article