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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Detalles Bibliográficos
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
Descripción
Sumario: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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