dc.contributor.author | Kocyigit, Umit M. | |
dc.contributor.author | Budak, Yakup | |
dc.contributor.author | Gurdere, Meliha Burcu | |
dc.contributor.author | Duru, Nese | |
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 | 2019-07-28T09:37:09Z | |
dc.date.available | 2019-07-27T12:10:23Z | |
dc.date.available | 2019-07-28T09:37:09Z | |
dc.date.issued | 2019 | |
dc.identifier.issn | 0026-9247 | |
dc.identifier.issn | 1434-4475 | |
dc.identifier.uri | https://dx.doi.org/10.1007/s00706-019-2350-z | |
dc.identifier.uri | https://hdl.handle.net/20.500.12418/5946 | |
dc.description | WOS: 000462504500015 | en_US |
dc.description.abstract | A series of novel 1,3,5-trisubstituted pyrazoline derivatives, (3aR,4S,7R,7aS)-2-[4-[1-acetyl-5-(aryl/heteroaryl)-4,5-dihydro-1H-pyrazol-3-yl]phenyl]-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindole-1,3(2H)-diones, were synthesized and evaluated for their antimicrobial and anticancer activities. In addition, the compounds were tested against acetylcholinesterase (AChE) enzyme and two physiologically relevant carbonic anhydrase I and II isozymes (hCA I and II). In this study, inhibition of hCA I and hCA II by the novel synthesized 1,3,5-trisubstituted pyrazolines was impressive, with K-i values in the range of 3.33-7.90nM for hCA I and 2.07-8.47nM for hCA II, while the K-i values of these compounds for AChE were recorded in the range of 9.61-48.42nM, respectively. Two compounds can be investigated as the leader compounds because of their lowest K-i values to make further detailed CA inhibition studies. [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 | SPRINGER WIEN | en_US |
dc.relation.isversionof | 10.1007/s00706-019-2350-z | en_US |
dc.rights | info:eu-repo/semantics/closedAccess | en_US |
dc.subject | Bioorganic chemistry | en_US |
dc.subject | Heterocyclics | en_US |
dc.subject | Enzyme inhibition | en_US |
dc.subject | Chalcone | en_US |
dc.subject | Antimicrobial | en_US |
dc.subject | Anticancer | en_US |
dc.title | Synthesis and investigation of anticancer, antibacterial activities and carbonic anhydrase, acetylcholinesterase inhibition profiles of novel (3aR,4S,7R,7aS)-2-[4-[1-acetyl-5-(aryl/heteroaryl)-4,5-dihydro-1H-pyrazol-3-yl]phenyl]-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindole-1,3(2H)-diones | en_US |
dc.type | article | en_US |
dc.relation.journal | MONATSHEFTE FUR CHEMIE | en_US |
dc.contributor.department | [Kocyigit, Umit M.] Cumhuriyet Univ, Vocat Sch Hlth Serv, TR-58140 Sivas, Turkey -- [Budak, Yakup -- Gurdere, Meliha Burcu -- Duru, Nese -- Ceylan, Mustafa] Gaziosmanpasa Univ, Fac Arts & Sci, Dept Chem, TR-60250 Tokat, Turkey -- [Taslimi, Parham -- Gulcin, Ilhami] Ataturk Univ, Fac Sci, Dept Chem, TR-25240 Erzurum, Turkey | en_US |
dc.identifier.volume | 150 | en_US |
dc.identifier.issue | 4 | en_US |
dc.identifier.endpage | 731 | en_US |
dc.identifier.startpage | 721 | en_US |
dc.relation.publicationcategory | Makale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı | en_US |