dc.contributor.author | Kocyigit, Umit M. | |
dc.contributor.author | Aslan, Osman Nuri | |
dc.contributor.author | Gulcin, Ilhami | |
dc.contributor.author | Temel, Yusuf | |
dc.contributor.author | Ceylan, Mustafa | |
dc.date.accessioned | 2019-07-27T12:10:23Z | |
dc.date.accessioned | 2019-07-28T09:44:32Z | |
dc.date.available | 2019-07-27T12:10:23Z | |
dc.date.available | 2019-07-28T09:44:32Z | |
dc.date.issued | 2016 | |
dc.identifier.issn | 0365-6233 | |
dc.identifier.issn | 1521-4184 | |
dc.identifier.uri | https://dx.doi.org/10.1002/ardp.201600092 | |
dc.identifier.uri | https://hdl.handle.net/20.500.12418/7099 | |
dc.description | WOS: 000392963000007 | en_US |
dc.description | PubMed ID: 27859585 | en_US |
dc.description.abstract | Carbonic anhydrase (CA, EC 4.2.1.1) is a member of the metalloenzyme family. It catalyzes the rapid conversion of carbon dioxide (CO2) and water to bicarbonate (HCO3-) and protons (H+) and also plays an important role in biochemical and physiological processes. In this study, a number of novel 2-(4-(aryl)thiazole-2-yl)-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindole-1,3(2H)-dione derivatives were synthesized and evaluated for their inhibitory characteristics against the human CA isoenzymes I and II (hCA I and hCA II). The structures of the new molecules 8a-i were confirmed by means of IR, H-1 NMR, C-13 NMR, and elemental analysis. These compounds exhibited excellent inhibitory effects, in the low nanomolar range, with K-i values in the range of 27.07-37.80 nM against hCA I and in the range of 11.80-25.81nM against hCA II. Our findings suggest that the new isoindolylthiazole derivatives have superior inhibitory effect over acetazolamide (AZA), which is used as clinical CA inhibitor with K-i values of 34.50 and 28.93nM against the hCA I and hCA II isoenzymes, respectively. | en_US |
dc.description.sponsorship | Department of Chemistry, Gaziosmanpasa University | en_US |
dc.description.sponsorship | The authors are grateful to the Department of Chemistry, Gaziosmanpasa University, for supports. | en_US |
dc.language.iso | eng | en_US |
dc.publisher | WILEY-V C H VERLAG GMBH | en_US |
dc.relation.isversionof | 10.1002/ardp.201600092 | en_US |
dc.rights | info:eu-repo/semantics/closedAccess | en_US |
dc.subject | Carbonic anhydrase | en_US |
dc.subject | Enzyme inhibition | en_US |
dc.subject | Isoindole | en_US |
dc.subject | Thiazole | en_US |
dc.title | Synthesis and Carbonic Anhydrase Inhibition of Novel 2-(4-(Aryl)thiazole-2-yl)-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindole-1,3(2H)-dione Derivatives | en_US |
dc.type | article | en_US |
dc.relation.journal | ARCHIV DER PHARMAZIE | en_US |
dc.contributor.department | [Kocyigit, Umit M.] Cumhuriyet Univ, Vocat Sch Hlth Serv, Sivas, Turkey -- [Aslan, Osman Nuri -- Ceylan, Mustafa] Gaziosmanpasa Univ, Fac Arts & Sci, Dept Chem, TR-60250 Tokat, Turkey -- [Gulcin, Ilhami] Ataturk Univ, Dept Chem, Fac Sci, Erzurum, Turkey -- [Gulcin, Ilhami] King Saud Univ, Dept Zool, Coll Sci, Riyadh, Saudi Arabia -- [Temel, Yusuf] Bingol Univ, Dept Solhan Sch Hlth Serv, Bingol, Turkey | en_US |
dc.contributor.authorID | GULCIN, Ilhami -- 0000-0001-5993-1668; ASLAN, Osman Nuri -- 0000-0002-1330-6194 | en_US |
dc.identifier.volume | 349 | en_US |
dc.identifier.issue | 12 | en_US |
dc.identifier.endpage | 963 | en_US |
dc.identifier.startpage | 955 | en_US |
dc.relation.publicationcategory | Makale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı | en_US |