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dc.contributor.authorEvranos-Aksoz, Begum
dc.contributor.authorYabanoglu-Ciftci, Samiye
dc.contributor.authorUcar, Gulberk
dc.contributor.authorYelekçi, Kemal
dc.contributor.authorErtan, Rahmiye
dc.date.accessioned2019-06-27T08:02:53Z
dc.date.available2019-06-27T08:02:53Z
dc.date.issued2014
dc.identifier.issn0960-894X
dc.identifier.issn1464-3405
dc.identifier.urihttps://hdl.handle.net/20.500.12469/703
dc.identifier.urihttps://doi.org/10.1016/j.bmcl.2014.06.015
dc.description.abstractA novel series of 2-pyrazoline and hydrazone derivatives were synthesized and investigated for their human monoamine oxidase (hMAO) inhibitory activity. All compounds inhibited the hMAO isoforms (MAO-A or MAO-B) competitively and reversibly. With the exception of 5i which was a selective MAO-B inhibitor all derivatives inhibited hMAO-A potently and selectively. According to the experimental K-i values compounds 6e and 6h exhibited the highest inhibitory activity towards the hMAO-A whereas compound 5j which carries a bromine atom at R-4 of the A ring of the pyrazoline appeared to be the most selective MAO-A inhibitor. Tested compounds were docked computationally into the active site of the hMAO-A and hMAO-B isozymes. The computationally obtained results were in good agreement with the corresponding experimental values. (C) 2014 Elsevier Ltd. All rights reserved.
dc.language.isoEnglish
dc.publisherPergamon-Elsevier Science Ltd
dc.rightsinfo:eu-repo/semantics/openAccessen_US
dc.subject2-Pyrazoline
dc.subjectHydrazone
dc.subjectMAO inhibitors
dc.subjectMolecular docking
dc.titleSynthesis of some novel hydrazone and 2-pyrazoline derivatives: Monoamine oxidase inhibitory activities and docking studies
dc.typeArticle
dc.identifier.startpage3278
dc.identifier.endpage3284
dc.relation.journalBioorganic & Medicinal Chemistry Letters
dc.identifier.issue15
dc.identifier.volume24
dc.identifier.wosWOS:000339228700012
dc.identifier.doi10.1016/j.bmcl.2014.06.015
dc.contributor.khasauthorYelekçi, Kemal


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