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Journal of Enzyme Inhibition and Medicinal Chemistry Volume 33, 2018 - Issue 1
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Short Communication

Carbonic anhydrases from Trypanosoma cruzi and Leishmania donovani chagasi are inhibited by benzoxaboroles

Alessio NocentiniInstitut des Biomolécules Max Mousseron (IBMM), UMR 5247 CNRS, ENSCM, Université de Montpellier, Montpellier Cedex, France; ;NEUROFARBA Department, Section of Pharmaceutical and Nutraceutical Sciences, University of Florence, Polo Scientifico, Firenze, ItalyView further author information
,
Roberta CadoniInstitut des Biomolécules Max Mousseron (IBMM), UMR 5247 CNRS, ENSCM, Université de Montpellier, Montpellier Cedex, France; View further author information
,
Pascal DumyInstitut des Biomolécules Max Mousseron (IBMM), UMR 5247 CNRS, ENSCM, Université de Montpellier, Montpellier Cedex, France; View further author information
,
Claudiu T. SupuranNEUROFARBA Department, Section of Pharmaceutical and Nutraceutical Sciences, University of Florence, Polo Scientifico, Firenze, ItalyView further author information
&
Jean-Yves WinumInstitut des Biomolécules Max Mousseron (IBMM), UMR 5247 CNRS, ENSCM, Université de Montpellier, Montpellier Cedex, France; Correspondence[email protected]
View further author information
Pages 286-289 | Received 08 Nov 2017, Accepted 05 Dec 2017, Published online: 27 Dec 2017
 
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Abstract

A series of 6-substituted ureido- and thioureido-benzoxaboroles were investigated as inhibitors of carbonic anhydrases from Trypanosoma cruzi (TcCA), and Leishmania donovani chagasi (LdcCA). Both enzymes were inhibited by benzoxaboroles in the micromolar range. Preferential inhibitory potency against the β-CA LdcCA versus the α-CA TcCA was observed with submicromolar inhibitory activities. Some derivatives displayed excellent inhibitory and selectivity profile over the ubiquitous and physiological relevant human off-target hCA II. This study provides a convincing opportunity to study benzoxaborole scaffold for the design of antiprotozoan potential drugs targeting the pathogen’s carbonic anhydrases.

Disclosure statement

The authors declare no conflict of interest.

Additional information

Funding

The authors thank the LabEx CheMISyst (ANR-10-LABX-05-01) (Agence Nationale de la Recherche) for funding.

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