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Journal of Enzyme Inhibition and Medicinal Chemistry Volume 32, 2017 - Issue 1
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Research Article

Carbonic anhydrase inhibitory properties of some uracil derivatives

Emir Alper TürkoğluDepartment of Pharmaceutical Technology, Agri Ibrahim Cecen University, Agri, Turkey;
,
Murat ŞentürkDepartment of Chemistry, Agri Ibrahim Cecen University, Agri, Turkey; Correspondence[email protected] [email protected]
,
Claudiu T. SupuranUniversità degli Studi di Firenze, Polo Scientifico, Laboratorio di Chimica Bioinorganica, Sesto Fiorentino, Florence, Italy; Correspondence[email protected] [email protected]
&
Deniz EkinciDepartment of Agricultural Biotechnology, Ondokuz Mayis University, Samsun, Turkey
Pages 74-77 | Received 15 Aug 2016, Accepted 07 Sep 2016, Published online: 18 Jan 2017
 
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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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