dc.contributor.author | Guney, Murat | |
dc.contributor.author | Cavdar, Huseyin | |
dc.contributor.author | Senturk, Murat | |
dc.contributor.author | Ekinci, Deniz | |
dc.date.accessioned | 2020-06-21T13:45:43Z | |
dc.date.available | 2020-06-21T13:45:43Z | |
dc.date.issued | 2015 | |
dc.identifier.issn | 0960-894X | |
dc.identifier.issn | 1464-3405 | |
dc.identifier.uri | https://doi.org/10.1016/j.bmcl.2015.05.073 | |
dc.identifier.uri | https://hdl.handle.net/20.500.12712/14160 | |
dc.description | Senturk, Murat/0000-0001-5968-7511 | en_US |
dc.description | WOS: 000357572000037 | en_US |
dc.description | PubMed: 26073005 | en_US |
dc.description.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 K-I values in the range of 10.83-464 mu M for hCA I and of 28.88-778.5 mu M 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. (C) 2015 Elsevier Ltd. All rights reserved. | en_US |
dc.description.sponsorship | Agri Ibrahim Cecen University Scientific Research CouncilAgri Ibrahim Cecen University [Agri BAP-2010/K-09]; TUBITAK (The Scientific and Technological Research Council of Turkey)Turkiye Bilimsel ve Teknolojik Arastirma Kurumu (TUBITAK) [114Z731] | en_US |
dc.description.sponsorship | This study was financed by Agri Ibrahim Cecen University Scientific Research Council, (project no: Agri BAP-2010/K-09) for (MG) and by TUBITAK (The Scientific and Technological Research Council of Turkey) (Project no: 114Z731) for (MS). The authors are grateful to Prof. Dr. Claudiu T. Supuran, University of Florence, for various valuable studies on carbonic anhydrase inhibitors. | en_US |
dc.language.iso | eng | en_US |
dc.publisher | Pergamon-Elsevier Science Ltd | en_US |
dc.relation.isversionof | 10.1016/j.bmcl.2015.05.073 | en_US |
dc.rights | info:eu-repo/semantics/closedAccess | en_US |
dc.subject | Carbonic anhydrase | en_US |
dc.subject | Hydroxyl | en_US |
dc.subject | Uracil | en_US |
dc.subject | Enzyme inhibitor | en_US |
dc.title | Synthesis and carbonic anhydrase inhibitory properties of novel uracil derivatives | en_US |
dc.type | article | en_US |
dc.contributor.department | OMÜ | en_US |
dc.identifier.volume | 25 | en_US |
dc.identifier.issue | 16 | en_US |
dc.identifier.startpage | 3261 | en_US |
dc.identifier.endpage | 3263 | en_US |
dc.relation.journal | Bioorganic & Medicinal Chemistry Letters | en_US |
dc.relation.publicationcategory | Makale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı | en_US |