Benzoxaborole as a new chemotype for carbonic anhydrase inhibition

Vincenzo Alterio; Roberta Cadoni; Davide Esposito; Daniela Vullo; Anna Di Fiore; Simona Maria Monti; Andrea Caporale; Menotti Ruvo; Mario Sechi; Pascal Dumy; Claudiu T. Supuran; Giuseppina De Simone; Jean-Yves Winum

doi:10.1039/C6CC06399C

Benzoxaborole as a new chemotype for carbonic anhydrase inhibition†

Vincenzo Alterio,‡^a Roberta Cadoni,‡^bc Davide Esposito,^a Daniela Vullo,^d Anna Di Fiore,^a Simona Maria Monti,^a Andrea Caporale,

^a Menotti Ruvo,^a Mario Sechi,^c Pascal Dumy,^b Claudiu T. Supuran,^e Giuseppina De Simone*^a and Jean-Yves Winum*^b

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* Corresponding authors

^a Istituto di Biostrutture e Bioimagini-CNR, Naples, Italy
E-mail: gdesimon@unina.it

^b Institut des Biomolécules Max Mousseron (IBMM) UMR5247 CNRS, ENSCM, Université de Montpellier, Montpellier, France
E-mail: jean-yves.winum@umontpellier.fr

^c Dipartimento di Chimica e Farmacia, Università degli Studi di Sassari, Sassari, Italy

^d Laboratorio di Chimica Bioinorganica, Polo Scientifico, Università degli Studi di Firenze, Sesto Fiorentino, Florence, Italy

^e Neurofarba Department, Section of Pharmaceutical and Nutriceutical Sciences, Università degli Studi di Firenze, Sesto Fiorentino, Florence, Italy

Abstract

In this paper we report the synthesis of a series of benzoxaborole derivatives, their inhibition properties against some carbonic anhydrases (CAs), recognized as important drug targets, and the characterization of the binding mode of these molecules to the CA active site. Our data provide the first experimental evidence that benzoxaboroles can be efficiently used as CA inhibitors.

Chemical Communications

Benzoxaborole as a new chemotype for carbonic anhydrase inhibition†

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