Carbonic anhydrase inhibitory properties of some uracil derivatives

Inhibitors of carbonic anhydrase (CA) have been carried out in many therapeutic applications, especially antiglaucoma activity. In this study, we investigated some uracil derivatives (4–12) to inhibit human CA I (hCA I) and II (hCA II) isoenzymes. The K(I) values of the compounds 4–12 are in the ran...

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Autores principales: Alper Türkoğlu, Emir, Şentürk, Murat, Supuran, Claudiu T., Ekinci, Deniz
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Taylor & Francis 2017
Materias:
Research Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6009904/
https://www.ncbi.nlm.nih.gov/pubmed/28097897
http://dx.doi.org/10.1080/14756366.2016.1235043
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author Alper Türkoğlu, Emir
Şentürk, Murat
Supuran, Claudiu T.
Ekinci, Deniz
author_facet Alper Türkoğlu, Emir
Şentürk, Murat
Supuran, Claudiu T.
Ekinci, Deniz
author_sort Alper Türkoğlu, Emir
collection PubMed
description Inhibitors of carbonic anhydrase (CA) have been carried out in many therapeutic applications, especially antiglaucoma activity. In this study, we investigated some uracil derivatives (4–12) to inhibit human CA I (hCA I) and II (hCA II) isoenzymes. The K(I) values of the compounds 4–12 are in the range of 0.085–428 µM for hCA I and of 0.1715–645 µM against hCA II, respectively. It is concluded from the kinetic investigations, all compounds used in the study act as competitive inhibitors with substrate, 4-NPA. Uracil derivatives are emerging agents for the inhibiton of carbonic anhydrase which could be used in biomedicine.
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spelling pubmed-60099042018-07-11 Carbonic anhydrase inhibitory properties of some uracil derivatives Alper Türkoğlu, Emir Şentürk, Murat Supuran, Claudiu T. Ekinci, Deniz J Enzyme Inhib Med Chem Research Article Inhibitors of carbonic anhydrase (CA) have been carried out in many therapeutic applications, especially antiglaucoma activity. In this study, we investigated some uracil derivatives (4–12) to inhibit human CA I (hCA I) and II (hCA II) isoenzymes. The K(I) values of the compounds 4–12 are in the range of 0.085–428 µM for hCA I and of 0.1715–645 µM against hCA II, respectively. It is concluded from the kinetic investigations, all compounds used in the study act as competitive inhibitors with substrate, 4-NPA. Uracil derivatives are emerging agents for the inhibiton of carbonic anhydrase which could be used in biomedicine. Taylor & Francis 2017-01-18 /pmc/articles/PMC6009904/ /pubmed/28097897 http://dx.doi.org/10.1080/14756366.2016.1235043 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 Research Article
Alper Türkoğlu, Emir
Şentürk, Murat
Supuran, Claudiu T.
Ekinci, Deniz
Carbonic anhydrase inhibitory properties of some uracil derivatives
title Carbonic anhydrase inhibitory properties of some uracil derivatives
title_full Carbonic anhydrase inhibitory properties of some uracil derivatives
title_fullStr Carbonic anhydrase inhibitory properties of some uracil derivatives
title_full_unstemmed Carbonic anhydrase inhibitory properties of some uracil derivatives
title_short Carbonic anhydrase inhibitory properties of some uracil derivatives
title_sort carbonic anhydrase inhibitory properties of some uracil derivatives
topic Research Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6009904/
https://www.ncbi.nlm.nih.gov/pubmed/28097897
http://dx.doi.org/10.1080/14756366.2016.1235043
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