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dc.contributor.authorSalgin-Goksen, Umut
dc.contributor.authorYabanoglu-Ciftci, Samiye
dc.contributor.authorErcan, Ayse
dc.contributor.authorYelekçi, Kemal
dc.contributor.authorUcar, Gulberk
dc.contributor.authorGokhan-Kelekçi, Nesrin
dc.date.accessioned2019-06-27T08:03:33Z
dc.date.available2019-06-27T08:03:33Z
dc.date.issued2013
dc.identifier.issn0300-9564
dc.identifier.issn1435-1463
dc.identifier.urihttps://hdl.handle.net/20.500.12469/806
dc.identifier.urihttps://dx.doi.org/10.1007/s00702-013-0980-6
dc.description.abstractA series of 1-[2-((5-methyl/chloro)-2-benzoxazolinone-3-yl)acetyl]-35-diaryl-45-dihydro-1H-pyrazole derivatives were prepared by reacting 2-((5-methyl/chloro)-2-benzoxazolinone-3-yl)acetylhydrazine with appropriate chalcones. The chemical structures of all compounds were confirmed by elemental analyses IR H-1 NMR and ESI-MS. All the compounds were investigated for their ability to selectively inhibit monoamine oxidase (MAO) by in vitro tests. MAO activities of the compounds were compared with moclobemide and selegiline and all the compounds were found to inhibit human MAO-A selectively. The inhibition profile was found to be competitive and reversible for all compounds by in vitro tests. Among the compounds examined compounds 5ae 5af and 5ag were more selective than moclobemide with respect to the K (i) values experimentally found. In addition the compound 5bg showed MAO-A inhibitor activity as well as moclobemide. A series of experimentally tested compounds (5ae-5ch) were docked computationally to the active site of the MAO-A and MAO-B isoenzyme. The AUTODOCK 4.01 program was employed to perform automated molecular docking.
dc.language.isoEnglish
dc.publisherSPRINGER WIEN
dc.rightsinfo:eu-repo/semantics/openAccessen_US
dc.subject2-Pyrazoline
dc.subject2-Benzoxazolinone
dc.subjectChalcone
dc.subjectMonoamine oxidase inhibitory activity
dc.subjectMolecular docking
dc.titleEvaluation of selective human MAO inhibitory activities of some novel pyrazoline derivatives
dc.typeArticle
dc.identifier.startpage863
dc.identifier.endpage873
dc.relation.journalJournal Of Neural Transmission
dc.identifier.issue6
dc.identifier.volume120
dc.identifier.wosWOS:000319433000005
dc.identifier.doi10.1007/s00702-013-0980-6
dc.contributor.khasauthorYelekçi, Kemal


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