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

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 agains...

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Autores principales: Nocentini, Alessio, Cadoni, Roberta, Dumy, Pascal, Supuran, Claudiu T., Winum, Jean-Yves
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Taylor & Francis 2017
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6009872/
https://www.ncbi.nlm.nih.gov/pubmed/29278948
http://dx.doi.org/10.1080/14756366.2017.1414808
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author Nocentini, Alessio
Cadoni, Roberta
Dumy, Pascal
Supuran, Claudiu T.
Winum, Jean-Yves
author_facet Nocentini, Alessio
Cadoni, Roberta
Dumy, Pascal
Supuran, Claudiu T.
Winum, Jean-Yves
author_sort Nocentini, Alessio
collection PubMed
description 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.
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spelling pubmed-60098722018-07-11 Carbonic anhydrases from Trypanosoma cruzi and Leishmania donovani chagasi are inhibited by benzoxaboroles Nocentini, Alessio Cadoni, Roberta Dumy, Pascal Supuran, Claudiu T. Winum, Jean-Yves J Enzyme Inhib Med Chem Short Communication 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. Taylor & Francis 2017-12-27 /pmc/articles/PMC6009872/ /pubmed/29278948 http://dx.doi.org/10.1080/14756366.2017.1414808 Text en © 2017 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group. http://creativecommons.org/licenses/by/4.0/ This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0/), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Short Communication
Nocentini, Alessio
Cadoni, Roberta
Dumy, Pascal
Supuran, Claudiu T.
Winum, Jean-Yves
Carbonic anhydrases from Trypanosoma cruzi and Leishmania donovani chagasi are inhibited by benzoxaboroles
title Carbonic anhydrases from Trypanosoma cruzi and Leishmania donovani chagasi are inhibited by benzoxaboroles
title_full Carbonic anhydrases from Trypanosoma cruzi and Leishmania donovani chagasi are inhibited by benzoxaboroles
title_fullStr Carbonic anhydrases from Trypanosoma cruzi and Leishmania donovani chagasi are inhibited by benzoxaboroles
title_full_unstemmed Carbonic anhydrases from Trypanosoma cruzi and Leishmania donovani chagasi are inhibited by benzoxaboroles
title_short Carbonic anhydrases from Trypanosoma cruzi and Leishmania donovani chagasi are inhibited by benzoxaboroles
title_sort carbonic anhydrases from trypanosoma cruzi and leishmania donovani chagasi are inhibited by benzoxaboroles
topic Short Communication
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6009872/
https://www.ncbi.nlm.nih.gov/pubmed/29278948
http://dx.doi.org/10.1080/14756366.2017.1414808
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