Inhibition of β-carbonic anhydrases from Brucella suis with C-cinnamoyl glycosides incorporating the phenol moiety

A small series of C-glycosides containing the phenol moiety was tested for the inhibition of the β-class carbonic anhydrases (βCAs, EC 4.2.1.1) from Brucella suis. Many compounds showed activities in the micromolar or submicromolar range and excellent selectivity for pathogen CAs over human isozymes...

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Autores principales: Riafrecha, Leonardo Ezequiel, Vullo, Daniela, Ouahrani-Bettache, Safia, Köhler, Stephan, Dumy, Pascal, Winum, Jean-Yves, Supuran, Claudiu T., Colinas, Pedro Alfonso
Formato: Articulo Comunicacion
Lenguaje:Inglés
Publicado: 2015
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Acceso en línea:http://sedici.unlp.edu.ar/handle/10915/123774
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Sumario:A small series of C-glycosides containing the phenol moiety was tested for the inhibition of the β-class carbonic anhydrases (βCAs, EC 4.2.1.1) from Brucella suis. Many compounds showed activities in the micromolar or submicromolar range and excellent selectivity for pathogen CAs over human isozymes. Glycosides incorporating the 3-hydroxyphenyl moiety showed the best inhibition profile, and therefore this functionality represents lead for the development of novel anti-infectives with a new mechanism of action.