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dc.contributor.authorYamali, Cem
dc.contributor.authorGul, Halise Inci
dc.contributor.authorKazaz, Cavit
dc.contributor.authorLevent, Serkan
dc.contributor.authorGulcin, Ilhami
dc.date.accessioned2020-07-09T20:58:43Z
dc.date.available2020-07-09T20:58:43Z
dc.date.issued2020
dc.identifier.issn0045-2068
dc.identifier.issn1090-2120
dc.identifier.urihttps://doi.org/10.1016/j.bioorg.2020.103627
dc.identifier.urihttps://hdl.handle.net/11421/23989
dc.descriptionWOS: 000516796900072en_US
dc.descriptionPubMed: 32058104en_US
dc.description.abstractA novel series of 4-(3-(difluorophenyl)-5-(dimethoxyphenyl)-4,5-dihydropyrazol-1-yl)benzenesulfonamides 1-8 were designed since sulfonamide and pyrazoline pharmacophores draw great attention in novel drug design due to their wide range of bioactivities including acetylcholinesterase (AChE) and human carbonic anhydrase I and II (hCA I and hCA II) inhibitory potencies. Comprehensive structure elucidation of the compounds synthesized was carried out by H-1 NMR, C-13 NMR, F-19 NMR, DEPT 90-135, H-1-H-1 COSY, H-1-C-13 HMQC, HMBC, and HRMS spectra. the chemical shifts and splitting patterns of the protons and carbons were affected by the fluorine atoms and exciting splitting patterns were also recorded for the fluorinated compounds. in vitro enzyme assays obviously showed that the novel compounds had a significant inhibitory profile against hCA I, hCA II and AChE enzymes at the nanomolar levels. Ki values were in the range of 3.30 +/- 1.09-5.95 +/- 2.26 nM for hCA I and 4.29 +/- 0.91-7.14 +/- 3.15 nM for hCA II, while Ki values for AChE were in the range of 3.28 +/- 1.47-9.77 +/- 1.86 nM. Many of thecompounds in this study can be considered as promising AChE and CA inhibitors.en_US
dc.description.sponsorshipAtaturk UniversityAtaturk University [2015/078]en_US
dc.description.sponsorshipThis study was financially supported by Ataturk University by the project 2015/078.en_US
dc.language.isoengen_US
dc.publisherAcademic Press Inc Elsevier Scienceen_US
dc.relation.isversionof10.1016/j.bioorg.2020.103627en_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.subjectPyrazolineen_US
dc.subjectSulfonamideen_US
dc.subjectFluorineen_US
dc.subjectCarbonic anhydraseen_US
dc.subjectAcetylcholinesteraseen_US
dc.titleSynthesis, structure elucidation, and in vitro pharmacological evaluation of novel polyfluoro substituted pyrazoline type sulfonamides as multi-target agents for inhibition of acetylcholinesterase and carbonic anhydrase I and II enzymesen_US
dc.typearticleen_US
dc.relation.journalBioorganic Chemistryen_US
dc.contributor.departmentAnadolu Üniversitesien_US
dc.identifier.volume96en_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US


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