dc.contributor.author | Budak, Yakup | |
dc.contributor.author | Kocyigit, Umit M. | |
dc.contributor.author | Gurdere, Meliha Burcu | |
dc.contributor.author | Ozcan, Kezban | |
dc.contributor.author | Taslimi, Parham | |
dc.contributor.author | Gulcin, Ilhami | |
dc.contributor.author | Ceylan, Mustafa | |
dc.date.accessioned | 2019-07-27T12:10:23Z | |
dc.date.accessioned | 2019-07-28T09:44:04Z | |
dc.date.available | 2019-07-27T12:10:23Z | |
dc.date.available | 2019-07-28T09:44:04Z | |
dc.date.issued | 2017 | |
dc.identifier.issn | 0039-7911 | |
dc.identifier.issn | 1532-2432 | |
dc.identifier.uri | https://dx.doi.org/10.1080/00397911.2017.1373406 | |
dc.identifier.uri | https://hdl.handle.net/20.500.12418/6889 | |
dc.description | WOS: 000418065300004 | en_US |
dc.description.abstract | Novel 4,5-dihydropyrazole derivatives (3a-i), 3-(4-((3aR,4S,7R,7aS)-1,3-dioxo-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindol-2(3H)-yl)phenyl)-5-phenyl-4,5-dihydro-1H-pyrazole-1-carbothio amide, were obtained by the addition of thiosemicarbazide (2) to the chalcones (1a-i). The addition-cyclization of 2,4-dibromoacetophenone (4) to pyrazole derivatives (3a-i) gave the new pyrazolyl-thiazole derivatives (5a-i), (3aR,4S,7R,7aS)-2-(4-(1-(4-(4-bromophenyl)thiazol-2-yl)-5-phenyl-4,5-dihydro-1H-pyrazol-3-yl)phenyl)-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindole-1,3(2H)-dione. Antibacterial and acetylcholinesterase (AChE) enzyme and human carbonic anhydrase (hCA) I, and II isoform inhibitory activities of the compounds 3a-i and 5a-i were investigated. Some of the compounds showed promising antibacterial activity. In addition, the hCA II and I were effectively inhibited by the lately synthesized derivatives, with K-i values in the range of 18.90 +/- 2.37 -58.25 +/- 13.62nM for hCA II and 5.72 +/- 0.98 -37.67 +/- 5.54nM for hCA I. Also, the K-i parameters of these compounds for AChE were obtained in the range of 25.47 +/- 11.11-255.74 +/- 82.20nM. Also, acetazolamide, clinical molecule, was used as a CA standard inhibitor that showed K-i value of 70.55 +/- 12.30nM against hCA II, and 67.17 +/- 9.1nM against hCA I, and tacrine inhibited AChE showed K-i value of 263.67 +/- 91.95. [GRAPHICS] . | en_US |
dc.description.sponsorship | Scientific and Technological Research Council of Turkey (TUBITAK) [111T990] | en_US |
dc.description.sponsorship | The authors are indebted to The Scientific and Technological Research Council of Turkey (TUBITAK Project No: 111T990) for financial supports. | en_US |
dc.language.iso | eng | en_US |
dc.publisher | TAYLOR & FRANCIS INC | en_US |
dc.relation.isversionof | 10.1080/00397911.2017.1373406 | en_US |
dc.rights | info:eu-repo/semantics/closedAccess | en_US |
dc.subject | Acetylcholinesterase | en_US |
dc.subject | antibacterial activity | en_US |
dc.subject | carbonic anhydrase | en_US |
dc.subject | pyrazole | en_US |
dc.subject | pyrazolyl-thiazole | en_US |
dc.title | Synthesis and investigation of antibacterial activities and carbonic anhydrase and acetyl cholinesterase inhibition profiles of novel 4,5-dihydropyrazol and pyrazolyl-thiazole derivatives containing methanoisoindol-1,3-dion unit | en_US |
dc.type | article | en_US |
dc.relation.journal | SYNTHETIC COMMUNICATIONS | en_US |
dc.contributor.department | [Budak, Yakup -- Gurdere, Meliha Burcu -- Ozcan, Kezban -- Ceylan, Mustafa] Gaziosmanpasa Univ, Fac Arts & Sci, Dept Chem, TR-60250 Tokat, Turkey -- [Kocyigit, Umit M.] Cumhuriyet Univ, Vocat Sch Hlth Serv, TR-58140 Sivas, Turkey -- [Taslimi, Parham -- Gulcin, Ilhami] Ataturk Univ, Dept Chem, Fac Sci, Erzurum, Turkey | en_US |
dc.contributor.authorID | GULCIN, Ilhami -- 0000-0001-5993-1668 | en_US |
dc.identifier.volume | 47 | en_US |
dc.identifier.issue | 24 | en_US |
dc.identifier.endpage | 2323 | en_US |
dc.identifier.startpage | 2313 | en_US |
dc.relation.publicationcategory | Makale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı | en_US |