Benzoxaboroles: New Potent Inhibitors of the Carbonic Anhydrases of the Pathogenic Bacterium Vibrio cholerae.

ABSTRACT: A series of urea/thiourea substituted benzoxaboroles was investigated for the inhibition of the three carbonic anhydrases encoded by Vibrio cholerae (VchCAα, VchCAβ, and VchCAγ). In particular, benzoxaborole derivatives were here first assayed for the inhibition of a γ-class CA, extending the panel of CA classes that benzoxaboroles efficiently target beyond α and β. Inhibition profiles demonstrated that VchCAα was significantly more inhibited compared to VchCAγ and, in turn, more efficiently modulated than VchCAβ. Among the many selective benzoxaborole ligands detected against VchCAα over the off-target hCA II, compound 18, a p-NO₂-phenylthiourea derivative, even exhibited a fully selective inhibition profile against the three VchCAs over hCA II. A comprehen

SUBMITTER: Bonardi A 

PROVIDER: S-EPMC7667823 | biostudies-literature | 2020 Nov

REPOSITORIES: biostudies-literature