dc.contributor.author | Ceylan, Mustafa | |
dc.contributor.author | Kocyigit, Umit M. | |
dc.contributor.author | Usta, Necibe Canan | |
dc.contributor.author | Gurbuzlu, Belma | |
dc.contributor.author | Temel, Yusuf | |
dc.contributor.author | Alwasel, Saleh H. | |
dc.contributor.author | Gulcin, Ilhami | |
dc.date.accessioned | 2019-07-27T12:10:23Z | |
dc.date.accessioned | 2019-07-28T09:41:37Z | |
dc.date.available | 2019-07-27T12:10:23Z | |
dc.date.available | 2019-07-28T09:41:37Z | |
dc.date.issued | 2017 | |
dc.identifier.issn | 1095-6670 | |
dc.identifier.issn | 1099-0461 | |
dc.identifier.uri | https://dx.doi.org/10.1002/jbt.21872 | |
dc.identifier.uri | https://hdl.handle.net/20.500.12418/6825 | |
dc.description | WOS: 000401253900001 | en_US |
dc.description | PubMed ID: 27780313 | en_US |
dc.description.abstract | Benzothiazepine compounds have a wide range of applications such as antibacterial, antidepressants, anticonvulsants, antihypertensives, antibiotics, antifungal, hypnotic, enzyme inhibitors, antitumor, anticancer and anti-HIV agents. In this study, the synthesis of novel tetralone-based benzothiazepine derivatives (1-16) and their in vitro antibacterial activity and human carbonic anhydrase isoenzymes I and II ( hCA I and II) inhibitory effects were investigated. Both isoenzymes were purified by sepharose-4B-L-tyrosine-sulfanilamide affinity chromatography from fresh human red blood cells. All compounds demonstrated the low nanomolar inhibitory effects on both isoenzymes using esterase activity. Benzothiazepine derivative 2 demonstrated the best hCA I inhibitory effect with Ki value of 18.19 nM. Also, benzothiazepine derivative 7 showed the best hCA II inhibitory effect with Ki value of 11.31 nM. On the other hand, acetazolamide clinically used as CA inhibitor, showed Ki value of 19.92 nM against hCA I and 33.60 nM against hCA II, respectively. | en_US |
dc.description.sponsorship | Gaziosmanpasa University, Scientific Research Projects Commission [BAP2014/33]; King Saud University | en_US |
dc.description.sponsorship | Contract Grant Sponsor: Gaziosmanpasa University, Scientific Research Projects Commission.; Contract Grant Number: BAP2014/33.; Contract Grant Sponsor: King Saud University. | en_US |
dc.language.iso | eng | en_US |
dc.publisher | WILEY | en_US |
dc.relation.isversionof | 10.1002/jbt.21872 | en_US |
dc.rights | info:eu-repo/semantics/closedAccess | en_US |
dc.subject | Antibacterial activity | en_US |
dc.subject | Benzothiazepine | en_US |
dc.subject | Carbonic anhydrase | en_US |
dc.subject | Enzyme purification | en_US |
dc.subject | Enzyme inhibition | en_US |
dc.title | Synthesis, carbonic anhydrase I and II isoenzymes inhibition properties, and antibacterial activities of novel tetralone-based 1,4-benzothiazepine derivatives | en_US |
dc.type | article | en_US |
dc.relation.journal | JOURNAL OF BIOCHEMICAL AND MOLECULAR TOXICOLOGY | en_US |
dc.contributor.department | [Ceylan, Mustafa -- Gurbuzlu, Belma] Gaziosmanpasa Univ, Fac Arts & Sci, Dept Chem, TR-60250 Tokat, Turkey -- [Kocyigit, Umit M.] Cumhuriyet Univ, Vocat Sch Hlth Serv, TR-58140 Sivas, Turkey -- [Usta, Necibe Canan] Gaziosmanpasa Univ, Fac Arts & Sci, Dept Biol, TR-60250 Tokat, Turkey -- [Temel, Yusuf] Bingol Univ, Dept Solhan, Sch Hlth Serv, TR-12000 Bingol, Turkey -- [Alwasel, Saleh H. -- Gulcin, Ilhami] King Saud Univ, Coll Sci, Dept Zool, Riyadh, Saudi Arabia -- [Gulcin, Ilhami] Ataturk Univ, Fac Sci, Dept Chem, TR-25240 Erzurum, Turkey | en_US |
dc.contributor.authorID | GULCIN, Ilhami -- 0000-0001-5993-1668 | en_US |
dc.identifier.volume | 31 | en_US |
dc.identifier.issue | 4 | en_US |
dc.relation.publicationcategory | Makale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı | en_US |