C-glycosides incorporating the 6-methoxy-2-naphthyl moiety are selective inhibitors of fungal and bacterial carbonic anhydrases

A small series of C-glycosides containing the methoxyaryl moieties was tested for the inhibition of the β-class carbonic anhydrases (CAs, EC 4.2.1.1) from <i>Cryptococcus neoformans</i> and <i>Brucella suis</i>. Many compounds showed activities in the micromolar or submicromo...

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Autores principales: Riafrecha, Leonardo Ezequiel, Vullo, Daniela, Supuran, Claudiu T., Colinas, Pedro Alfonso
Formato: Articulo
Lenguaje:Inglés
Publicado: 2014
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Acceso en línea:http://sedici.unlp.edu.ar/handle/10915/124089
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Sumario:A small series of C-glycosides containing the methoxyaryl moieties was tested for the inhibition of the β-class carbonic anhydrases (CAs, EC 4.2.1.1) from <i>Cryptococcus neoformans</i> and <i>Brucella suis</i>. Many compounds showed activities in the micromolar or submicromolar range and excellent selectivity for pathogen CAs over human isozymes. The deprotected glycosides incorporating the 6-methoxy-2-naphthyl moiety showed the best inhibition profile and therefore represent leads for the development of novel anti-infectives with a new mechanism of action.