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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...
Autores principales: | , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Taylor & Francis
2017
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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. |
format | Online Article Text |
id | pubmed-6009872 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2017 |
publisher | Taylor & Francis |
record_format | MEDLINE/PubMed |
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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