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 KI 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.
Carbonic anhydrase inhibitory properties of some uracil derivatives / Alper Türkoğlu, Emir; Şentürk, Murat; Supuran, Claudiu T; Ekinci, Deniz. - In: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY. - ISSN 1475-6366. - STAMPA. - 32:(2017), pp. 74-77. [10.1080/14756366.2016.1235043]
Carbonic anhydrase inhibitory properties of some uracil derivatives
SUPURAN, CLAUDIU TRANDAFIR;
2017
Abstract
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 KI 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.I documenti in FLORE sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.