Synthesis, anticonvulsant and antimicrobial activities of some new 2-acetylnaphthalene derivatives

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dc.authoridKarakurt, Arzu/0000-0003-2209-0871
dc.authorwosidKarakurt, Arzu/ABH-9340-2020
dc.contributor.authorKarakurt, Arzu
dc.contributor.authorOzalp, Meral
dc.contributor.authorIsik, Samil
dc.contributor.authorStables, James P.
dc.contributor.authorDalkara, Sevim
dc.date.accessioned2024-08-04T21:01:17Z
dc.date.available2024-08-04T21:01:17Z
dc.date.issued2010
dc.departmentİnönü Üniversitesien_US
dc.description.abstractIn this study, as a continuation of our research for new (arylalkyl) imidazole anticonvulsant compounds, the design, synthesis and anticonvulsant/antimicrobial activity evaluation of a series of 2-acetylnaphthalene derivatives have been described. Molecular design of the compounds has been based on the modification of nafimidone [1-(2-naphthyl)-2-(imidazol-1-yl)ethanone], which is a representative of the (arylalkyl) imidazole anticonvulsant compounds as well as its active metabolite, nafimidone alcohol (3, 4). In general, these compounds were variously substituted at the alkyl chain between naphthalene and imidazole rings and subjected to some other modifications to evaluate additional structure-activity relationships. The anticonvulsant activity profile of those compounds was determined by maximal electroshock seizure (MES) and subcutaneous metrazol (scM) seizure tests, whereas their neurotoxicity was examined using rotarod test. All the ester derivatives of nafimidone alcohol (5a-h), which were designed as prodrugs, showed anticonvulsant activity against MES-induced seizure model. Four of the most active compounds were chosen for further anticonvulsant evaluations. Quantification of anticonvulsant protection was calculated via the ip route (ED(50) and TD(50)) for the most active candidate (5d). Observed protection in the MES model was 38.46 mg kg (1) and 123.83 mg kg (1) in mice and 20.44 mg kg (1), 56.36 mg kg (1) in rats, respectively. Most of the compounds with imidazole ring also showed antibacterial and/ or antifungal activities to a certain extent in addition to their anticonvulsant activity. (C) 2010 Elsevier Ltd. All rights reserved.en_US
dc.description.sponsorshipHacettepe University [HUBAB 02 02 301 002]en_US
dc.description.sponsorshipThis project was supported by Hacettepe University Scientific Research Fund (HUBAB 02 02 301 002).en_US
dc.identifier.doi10.1016/j.bmc.2010.03.010
dc.identifier.endpage2911en_US
dc.identifier.issn0968-0896
dc.identifier.issue8en_US
dc.identifier.pmid20363141en_US
dc.identifier.startpage2902en_US
dc.identifier.urihttps://doi.org/10.1016/j.bmc.2010.03.010
dc.identifier.urihttps://hdl.handle.net/11616/104251
dc.identifier.volume18en_US
dc.identifier.wosWOS:000276528700010en_US
dc.identifier.wosqualityQ2en_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakPubMeden_US
dc.language.isoenen_US
dc.publisherPergamon-Elsevier Science Ltden_US
dc.relation.ispartofBioorganic & Medicinal Chemistryen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.subject2-Acetylnaphthaleneen_US
dc.subject(Arylalkyl)imidazoleen_US
dc.subjectAntimicrobial activityen_US
dc.subjectAnticonvulsant activityen_US
dc.titleSynthesis, anticonvulsant and antimicrobial activities of some new 2-acetylnaphthalene derivativesen_US
dc.typeArticleen_US

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