(Hetero)aryl substituted thiazol-2,4-yl scaffold as human carbonic anhydrase I, II, VII and XIV activators

Using histamine as lead molecule, a library of (hetero)aryl substituted thiazol-2,4-yl derivatives incorporating pyridine as proton shuttling moiety were obtained and investigated as activators of human carbonic anhydrase (CA, EC 4.2.1.1) isoforms I, II, VII and XIV. Some derivatives displayed good...

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Autores principales: Rami, Marouan, Winum, Jean-Yves, Supuran, Claudiu T., Melnyk, Patricia, Yous, Saïd
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Taylor & Francis 2019
Materias:
Research Paper
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6327990/
https://www.ncbi.nlm.nih.gov/pubmed/30734616
http://dx.doi.org/10.1080/14756366.2018.1543292
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author Rami, Marouan
Winum, Jean-Yves
Supuran, Claudiu T.
Melnyk, Patricia
Yous, Saïd
author_facet Rami, Marouan
Winum, Jean-Yves
Supuran, Claudiu T.
Melnyk, Patricia
Yous, Saïd
author_sort Rami, Marouan
collection PubMed
description Using histamine as lead molecule, a library of (hetero)aryl substituted thiazol-2,4-yl derivatives incorporating pyridine as proton shuttling moiety were obtained and investigated as activators of human carbonic anhydrase (CA, EC 4.2.1.1) isoforms I, II, VII and XIV. Some derivatives displayed good activating and selectivity profiles. This study provides an interesting opportunity to study the thiazole scaffold for the design of CA activators (CAAs), possibly acting on the central nervous system and targeting pathologies involving memory and learning impairments.
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spelling pubmed-63279902019-01-16 (Hetero)aryl substituted thiazol-2,4-yl scaffold as human carbonic anhydrase I, II, VII and XIV activators Rami, Marouan Winum, Jean-Yves Supuran, Claudiu T. Melnyk, Patricia Yous, Saïd J Enzyme Inhib Med Chem Research Paper Using histamine as lead molecule, a library of (hetero)aryl substituted thiazol-2,4-yl derivatives incorporating pyridine as proton shuttling moiety were obtained and investigated as activators of human carbonic anhydrase (CA, EC 4.2.1.1) isoforms I, II, VII and XIV. Some derivatives displayed good activating and selectivity profiles. This study provides an interesting opportunity to study the thiazole scaffold for the design of CA activators (CAAs), possibly acting on the central nervous system and targeting pathologies involving memory and learning impairments. Taylor & Francis 2019-01-03 /pmc/articles/PMC6327990/ /pubmed/30734616 http://dx.doi.org/10.1080/14756366.2018.1543292 Text en © 2018 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 Research Paper
Rami, Marouan
Winum, Jean-Yves
Supuran, Claudiu T.
Melnyk, Patricia
Yous, Saïd
(Hetero)aryl substituted thiazol-2,4-yl scaffold as human carbonic anhydrase I, II, VII and XIV activators
title (Hetero)aryl substituted thiazol-2,4-yl scaffold as human carbonic anhydrase I, II, VII and XIV activators
title_full (Hetero)aryl substituted thiazol-2,4-yl scaffold as human carbonic anhydrase I, II, VII and XIV activators
title_fullStr (Hetero)aryl substituted thiazol-2,4-yl scaffold as human carbonic anhydrase I, II, VII and XIV activators
title_full_unstemmed (Hetero)aryl substituted thiazol-2,4-yl scaffold as human carbonic anhydrase I, II, VII and XIV activators
title_short (Hetero)aryl substituted thiazol-2,4-yl scaffold as human carbonic anhydrase I, II, VII and XIV activators
title_sort (hetero)aryl substituted thiazol-2,4-yl scaffold as human carbonic anhydrase i, ii, vii and xiv activators
topic Research Paper
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6327990/
https://www.ncbi.nlm.nih.gov/pubmed/30734616
http://dx.doi.org/10.1080/14756366.2018.1543292
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