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 rang...

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Veröffentlicht in:Journal of enzyme inhibition and medicinal chemistry 2017-01, Vol.32 (1), p.74-77
Hauptverfasser: Alper Türkoğlu, Emir, Şentürk, Murat, Supuran, Claudiu T., Ekinci, Deniz
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Sprache:eng
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Zusammenfassung: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.
ISSN:1475-6366
1475-6374
DOI:10.1080/14756366.2016.1235043