dc.contributor.author | Kocyigit-Kaymakcioglu, Bedia | |
dc.contributor.author | Aker, Rezzan Gulhan | |
dc.contributor.author | Tezcan, Kutluhan | |
dc.contributor.author | Sakalli, Eren | |
dc.contributor.author | Ketenci, Sema | |
dc.contributor.author | Oruc-Emre, Emine Elcin | |
dc.contributor.author | Rollas, Sevim | |
dc.date.accessioned | 2019-08-13T12:10:23Z | |
dc.date.accessioned | 2019-08-13T16:04:09Z | |
dc.date.available | 2019-08-13T12:10:23Z | |
dc.date.available | 2019-08-13T16:04:09Z | |
dc.date.issued | 2011 | |
dc.identifier.issn | 1054-2523 | |
dc.identifier.uri | https://dx.doi.org/10.1007/s00044-010-9358-6 | |
dc.identifier.uri | http://hdl.handle.net/11446/3245 | |
dc.description | WOS: 000289849900012 | en_US |
dc.description.abstract | A series of 3,5-dimethylpyrazole derivatives, structurally related to the previously described potent ameltolide analogues, were synthesized and evaluated for their anticonvulsant activity. Ten compounds were prepared by reacting the 4-amino-3,5-dimethylpyrazole with appropriate substituted carboxylic acids, benzoyl chlorides and benzaldehydes to obtain amide and imine derivatives. Initial anticonvulsant screening was performed using intraperitoneal pentylenetetrazole (PTZ) and maximal electroshock (MES) induced seizure tests in mice. Among the 10 tested compounds, N-[1-(4-methoxybenzoyl)-3,5-dimethylpyrazole-4-yl]-4-methoxybenzamide 2 and N-[1-(2,6-dichlorobenzoyl)-3,5-dimethylpyrazole-4-yl]-2,6-dichlorobenzamide 3 decreased seizure severity and the mortality rate in the PTZ test. Hence, compound 3 was tested in an animal model of absence epilepsy, Genetic Absence Epileptic Rats from Strasbourg (GAERS). There were no significant changes in the duration or number of spike-and-wave discharges in this model. | en_US |
dc.description.sponsorship | Marmara University Scientific Research Projects Commission (BAPKO) [SAG-BGS-270605-0132] | en_US |
dc.description.sponsorship | The authors thank Marmara University Scientific Research Projects Commission (BAPKO, Project number SAG-BGS-270605-0132) for the financial support of this study and to Prof. R.W. Guillery for his valuable comments on the manuscript. | en_US |
dc.language.iso | eng | en_US |
dc.publisher | BIRKHAUSER BOSTON INC | en_US |
dc.identifier.doi | 10.1007/s00044-010-9358-6 | en_US |
dc.rights | info:eu-repo/semantics/closedAccess | en_US |
dc.subject | 3,5-Dimethylpyrazole | en_US |
dc.subject | Amide | en_US |
dc.subject | Imine | en_US |
dc.subject | Anticonvulsant activity | en_US |
dc.title | Anticonvulsant activity of 3,5-dimethylpyrazole derivatives in animal models | en_US |
dc.type | article | en_US |
dc.relation.journal | MEDICINAL CHEMISTRY RESEARCH | en_US |
dc.department | DBÜ | en_US |
dc.identifier.issue | 5 | en_US |
dc.identifier.volume | 20 | en_US |
dc.identifier.startpage | 607 | en_US |
dc.identifier.endpage | 614 | en_US |
dc.contributor.authorID | 0000-0003-4601-7871 | en_US |
dc.contributor.authorID | 0000-0003-0680-4782 | en_US |
dc.contributor.authorID | 0000-0002-1519-3170 | en_US |
dc.relation.publicationcategory | Makale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı | en_US |
dc.department-temp | [Kocyigit-Kaymakcioglu, Bedia -- Rollas, Sevim] Marmara Univ, Fac Pharm, Dept Pharmaceut Chem, TR-34668 Istanbul, Turkey -- [Aker, Rezzan Gulhan -- Tezcan, Kutluhan -- Sakalli, Eren -- Ketenci, Sema -- Gurbanova, Ayten -- Terzioglu, Berna -- Onat, Filiz] Marmara Univ, Sch Med, Dept Pharmacol & Clin Pharmacol, TR-34668 Istanbul, Turkey -- [Oruc-Emre, Emine Elcin] Gaziantep Univ, Dept Chem, Sehitkamil, Gaziantep, Turkey -- [Akin, Demet] Istanbul Bilim Univ, Sch Med, Dept Pharmacol, Istanbul, Turkey -- [Kocyigit-Kaymakcioglu, Bedia -- Aker, Rezzan Gulhan -- Oruc-Emre, Emine Elcin -- Onat, Filiz -- Rollas, Sevim] Marmara Univ, Epilepsy Res Ctr, TR-34668 Istanbul, Turkey | en_US |