Carbonic anhydrase inhibitory properties of some uracil derivatives

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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.

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Alper Türkoğlu, E., Şentürk, M., Supuran, C. T., & Ekinci, D. (2017). Carbonic anhydrase inhibitory properties of some uracil derivatives. Journal of Enzyme Inhibition and Medicinal Chemistry, 32(1), 74–77. https://doi.org/10.1080/14756366.2016.1235043

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