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dc.contributor.authorSalgın-Göksen, Umut
dc.contributor.authorTelli, Gökçen
dc.contributor.authorErikci, Açelya
dc.contributor.authorDedecengiz, Ezgi
dc.contributor.authorTel, Banu Cahide
dc.contributor.authorKaynak, F. Betül
dc.contributor.authorYelekçi, Kemal
dc.contributor.authorÜcar, Gülberk
dc.contributor.authorGökhan-Kelekçi, Nesrin
dc.date.accessioned2021-04-24T16:48:23Z
dc.date.available2021-04-24T16:48:23Z
dc.date.issued2021-02
dc.identifier.issn0022-2623
dc.identifier.urihttps://hdl.handle.net/20.500.12469/4002
dc.description.abstractThirty compounds having 1-[2-(5-substituted-2-benzoxazolinone-3-yl) acetyl]-3,5-disubstitutedphenyl-2-pyrazoline structure and nine compounds having N'-(1,3-disubstitutedphenylallylidene)-2-(5-substituted- 2-benzoxazolinone-3-yl)-acetohydrazide skeleton were synthesized and evaluated as monoamine oxidase (MAO) inhibitors. All of the compounds exhibited selective MAO-A inhibitor activity in the nanomolar or low micromolar range. The results of the molecular docking for hydrazone derivatives supported the in vitro results. Five compounds, 6 (0.008 mu M, Selectivity Index (SI): 9.70 x 10(-4)), 7 (0.009 mu M, SI: 4.55 x 10(-5)), 14 (0.001 mu M, SI: 8.00 x 10(-4)), 21 (0.009 mu M, SI: 1.37 x 10(-5)), and 42 (0.010 mu M, SI: 5.40 x 10(-6)), exhibiting the highest inhibition and selectivity toward hMAO-A and nontoxic to hepatocytes were assessed for antidepressant activity as acute and subchronic in mice. All of these five compounds showed significant antidepressant activity with subchronic administration consistent with the increase in the brain serotonin levels and the compounds crossed the blood-brain barrier according to parallel artificial membrane permeation assay. Compounds 14, 21, and 42 exhibited an ex vivo MAO-A profile, which is highly consistent with the in vitro data.en_US
dc.language.isoEnglishen_US
dc.publisherAMER CHEMICAL SOCen_US
dc.subjectCRYSTAL-STRUCTURESen_US
dc.titleNew 2-Pyrazoline and Hydrazone Derivatives as Potent and Selective Monoamine Oxidase A Inhibitorsen_US
dc.typeArticleen_US
dc.identifier.startpage1989en_US
dc.identifier.endpage2009en_US
dc.relation.journalJOURNAL OF MEDICINAL CHEMISTRYen_US
dc.identifier.issue4en_US
dc.identifier.volume64en_US
dc.identifier.wos000624369300013en_US
dc.identifier.doi10.1021/acs.jmedchem.0c01504en_US
dc.contributor.khasauthorYelekçi, Kemalen_US


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