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Bioorg Med Chem Lett. 2015 Aug 15;25(16):3261-3. doi: 10.1016/j.bmcl.2015.05.073. Epub 2015 May 30.

Synthesis and carbonic anhydrase inhibitory properties of novel uracil derivatives.

Author information

1
Ağrı İbrahim Çeçen University, Department of Chemistry, 04100 Ağrı, Turkey. Electronic address: mguney@agri.edu.tr.
2
Dumlupinar University, Education Faculty, 43100 Kutahya, Turkey.
3
Ağrı İbrahim Çeçen University, Department of Chemistry, 04100 Ağrı, Turkey. Electronic address: msenturk@agri.edu.tr.
4
Ondokuz Mayıs University, Department of Agricultural Biotechnology, 55139 Samsun, Turkey.

Abstract

Carbonic anhydrase (CA) inhibitors are valuable molecules based on several therapeutic applications, including antiglaucoma activity. In the present study, inhibition of two human cytosolic carbonic anhydrase isozymes I and II with some uracil derivatives (3-9) were investigated. Compounds 3-9 showed KI values in the range of 10.83-464 μM for hCA I and of 28.88-778.5 μM against hCA II, respectively. Kinetic investigations showed that similarly to classical CA inhibitors, all investigated natural compounds act as competitive inhibitors with 4-NPA as substrate. Uracil derivatives investigated here are promising agents which may be used as lead molecules in order to derivative novel carbonic anhydrase inhibitors that might be useful in medical applications.

KEYWORDS:

Carbonic anhydrase; Enzyme inhibitor; Hydroxyl; Uracil

PMID:
26073005
DOI:
10.1016/j.bmcl.2015.05.073
[Indexed for MEDLINE]

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