Synthesis, anticonvulsant activity, and molecular modeling studies of novel 1-phenyl/1-(4-chlorophenyl)-2-(1H-triazol-1-yl)ethanol ester derivatives

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dc.authoriddogan, inci selin/0000-0003-4949-1747
dc.authoridSARI, SUAT/0000-0002-8248-4218
dc.authoridOzdemir, Zenyep/0000-0003-4559-2305
dc.authoridSARI, SUAT/0000-0002-8248-4218
dc.authoridBozbey Merde, İrem/0000-0002-9290-938X
dc.authoridKarakurt, Arzu/0000-0003-2209-0871
dc.authorwosiddogan, inci selin/AAR-4150-2020
dc.authorwosidSARI, SUAT/JCD-8070-2023
dc.authorwosidOzdemir, Zenyep/AAJ-6384-2020
dc.authorwosidSARI, SUAT/A-5249-2017
dc.authorwosidBozbey Merde, İrem/HCI-8239-2022
dc.authorwosidKarakurt, Arzu/ABH-9340-2020
dc.contributor.authorDogan, Inci Selin
dc.contributor.authorOzdemir, Zeynep
dc.contributor.authorSari, Suat
dc.contributor.authorBozbey, Irem
dc.contributor.authorKarakurt, Arzu
dc.contributor.authorSarac, Selma
dc.date.accessioned2024-08-04T20:45:22Z
dc.date.available2024-08-04T20:45:22Z
dc.date.issued2018
dc.departmentİnönü Üniversitesien_US
dc.description.abstractA series of new ester derivatives were synthesized by the reaction of various acids with 1-phenyl/1-(4-chlorophenyl)-2-(1H-triazol-1-yl)ethanol and in vivo screened for their anticonvulsant activity. The title compounds were screened against MES and ScM seizure tests according to a modified version of the Epilepsy Therapy Screening Program (ETSP) protocol of the National Institutes of Health (NIH). Their neurotoxic effects were evaluated by the rotarod test. All the compounds showed protection against MES and/or ScM-induced seizures at 30 mg/kg without neurotoxicity. More compounds were found active in the ScM test and at lower dose than the MES test. Physicochemical and pharmacokinetic profiles of the compounds were predicted by QikProp. Using molecular docking approach we tried to get insights into their possible anticonvulsant mechanisms.en_US
dc.description.sponsorshipScientific and Technological Research Council of Turkey (TUBITAK) [114S862]en_US
dc.description.sponsorshipThis research was financially supported by The Scientific and Technological Research Council of Turkey (TUBITAK) (Grant no: 114S862). This study has been partly presented on International Conference on Pharmaceutical Chemistry, 5-8 September 2016, Frankfurt-Germany as a poster presentation with title of Synthesis and anticonvulsant activities of novel 1-phenyl/1-(4-chlorophenyl)- 2-(1H-triazol-1-yl) ethanol ester derivative compounds.en_US
dc.identifier.doi10.1007/s00044-018-2225-6
dc.identifier.endpage2186en_US
dc.identifier.issn1054-2523
dc.identifier.issn1554-8120
dc.identifier.issue9en_US
dc.identifier.scopus2-s2.0-85051465825en_US
dc.identifier.scopusqualityQ2en_US
dc.identifier.startpage2171en_US
dc.identifier.urihttps://doi.org/10.1007/s00044-018-2225-6
dc.identifier.urihttps://hdl.handle.net/11616/98427
dc.identifier.volume27en_US
dc.identifier.wosWOS:000442575300012en_US
dc.identifier.wosqualityQ4en_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakScopusen_US
dc.language.isoenen_US
dc.publisherSpringer Birkhauseren_US
dc.relation.ispartofMedicinal Chemistry Researchen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.subjectAnticonvulsant activityen_US
dc.subject(Arylalkyl)azolesen_US
dc.subjectEsteren_US
dc.subjectMolecular dockingen_US
dc.subjectSynthesisen_US
dc.subjectTriazoleen_US
dc.titleSynthesis, anticonvulsant activity, and molecular modeling studies of novel 1-phenyl/1-(4-chlorophenyl)-2-(1H-triazol-1-yl)ethanol ester derivativesen_US
dc.typeArticleen_US

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