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dc.contributor.authorGökhan, N
dc.contributor.authorYeşilada, A
dc.contributor.authorUçar, G
dc.contributor.authorErol, K
dc.contributor.authorBilgin, AA
dc.date.accessioned2019-10-22T20:08:19Z
dc.date.available2019-10-22T20:08:19Z
dc.date.issued2003
dc.identifier.issn0365-6233
dc.identifier.urihttps://dx.doi.org/10.1002/ardp.200300732
dc.identifier.urihttps://hdl.handle.net/11421/22532
dc.descriptionWOS: 000185327300002en_US
dc.descriptionPubMed ID: 14502756en_US
dc.description.abstractTwelve new 1-N-substituted thiocarbomoyl-3-phehyl-5-thienyl-2-pyrazoline derivatives were synthesized and evaluated their for antidepressant, anxiogenic and mammalian monoamine oxidase (MAO)-A and B inhibitory activities by in vivo and in vitro tests. MAO was isolated and purified from the mitochondrial pellet of bovine liver homogenates and human platelets. All of the new compounds inhibited the total MAO activity of liver homogenates and the inhibition was found to be time-dependent. Four compounds (3 i-3 I) inhibited MAO-B selectively and irreversibly in a classical non-competitive manner with IC50 values in the range of 22.00-91.50 muM. The rest of the compounds appeared to be non-selective reversible inhibitors. It was suggested that the p-methoxy group on the phenyl ring in the compounds increased the inhibitory effect and selectivity toward MAO-B. The reversible and unselective inhibition of MAO by the remaining compounds was suggested to be related to their properties of actingability to act as both as substrate and inhibitor at the same time. However, none of the novel compounds showed antidepressant activity as expected suggesting formation of inactive metabolites. We conclude that the compounds appeared as which functioned as selective MAO-B inhibitors might have promising features as therapeutic properties in the treatment of Parkinson disease. In vivo studies are needed to verify this hypothesis.en_US
dc.language.isoengen_US
dc.publisherWiley-V C H Verlag GMBHen_US
dc.relation.isversionof10.1002/ardp.200300732en_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.subjectMonoamine Oxidaseen_US
dc.subjectMonoamine Monoamine Oxidase Inhibitorsen_US
dc.subjectN-Subtituted Subtituted 2-Pyrazoline Derivativesen_US
dc.title1-N-substituted thiocarbamoyl-3-phenyl-5-thienyl-2-pyrazolines: Synthesis and evaluation as MAO inhibitorsen_US
dc.typearticleen_US
dc.relation.journalArchiv Der Pharmazieen_US
dc.contributor.departmentAnadolu Üniversitesi, Tıp Fakültesi, Farmakoloji Anabilim Dalıen_US
dc.identifier.volume336en_US
dc.identifier.issue8en_US
dc.identifier.startpage362en_US
dc.identifier.endpage371en_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US]


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