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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 comprehensive ligand/target interaction study was performed in silico for all three VchCA isoforms providing the first molecular modeling investigation with inhibitors of a γ-class CA to the best of our knowledge. The present study reinforces the rationale behind the use of benzoxaboroles as innovative antibacterial agents with a new mechanism of action, furnishing suggestions for the rational design of new potent and selective inhibitors targeting V. cholerae CAs over human off-target ones.

journal_name

ACS Med Chem Lett

journal_title

ACS medicinal chemistry letters

authors

Bonardi A,Nocentini A,Cadoni R,Del Prete S,Dumy P,Capasso C,Gratteri P,Supuran CT,Winum JY

doi

10.1021/acsmedchemlett.0c00403

subject

Has Abstract

pub_date

2020-09-09 00:00:00

pages

2277-2284

issue

11

issn

1948-5875

journal_volume

11

pub_type

杂志文章

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