Novel 4-thiazolidinone derivatives as agonists of benzodiazepine receptors
| dc.contributor.author | Faizi, Mehrdad | |
| dc.contributor.author | Jahani, Reza | |
| dc.contributor.author | Ebadi, Seyed Abbas | |
| dc.contributor.author | Tabatabai, Sayyed Abbas | |
| dc.contributor.author | Rezaee, Elham | |
| dc.contributor.author | Lotfaliei, Mehrnaz | |
| dc.contributor.author | Amini, Mohsen | |
| dc.contributor.author | Almasirad, Ali | |
| dc.date.accessioned | 2017-05-03T14:00:29Z | |
| dc.date.available | 2017-05-03T14:00:29Z | |
| dc.date.issued | 2017-01-13 | |
| dc.description.abstract | A new series of 4-chloro-N-(2-(substitutedphenyl)-4-oxothiazolidin-3-yl)-2-phenoxybenzamide derivatives were designed, synthesized and biologically evaluated as anticonvulsant agents. The designed compounds have the main essential functional groups for binding to the benzodiazepine receptors and 4-thiazolidinone ring as an anticonvulsant pharmacophore. Some of the new synthesized compounds showed considerable anticonvulsant activity in electroshock and pentylenetetrazole-induced lethal convulsion tests. Compound 5i, 4-chloro-N-(2-(4-methoxyphenyl)-4-oxothiazolidin-3-yl)-2-phenoxybenzamide, with the best activity was selected for evaluation of other benzodiazepine pharmacological effects. This compound induced significant sedative-hypnotic activity. However, it does not impair the learning and memory in the experimental condition. Flumazenil was able to antagonize the sedative-hypnotic and anticonvulsant effects of compound 5i indicating that benzodiazepine receptors are highly involved in the pharmacological properties of the novel compounds. | en |
| dc.identifier.doi | 10.17179/excli2016-692 | |
| dc.identifier.issn | 1611-2156 | |
| dc.identifier.uri | http://hdl.handle.net/2003/35950 | |
| dc.identifier.uri | http://dx.doi.org/10.17877/DE290R-17973 | |
| dc.language.iso | en | |
| dc.relation.ispartofseries | EXCLI Journal;Vol. 16 2017 | |
| dc.rights.uri | http://creativecommons.org/licenses/by/4.0/ | |
| dc.subject | benzodiazepine | en |
| dc.subject | sedative-hypnotic | en |
| dc.subject | anticonvulsant | en |
| dc.subject | 4-thiazolidinone derivatives | en |
| dc.subject | synthesis | en |
| dc.subject.ddc | 610 | |
| dc.title | Novel 4-thiazolidinone derivatives as agonists of benzodiazepine receptors | en |
| dc.title.alternative | Design, synthesis and pharmacological evaluation | en |
| dc.type | Text | |
| dc.type.publicationtype | article | |
| dcterms.accessRights | open access | |
| eldorado.dnb.deposit | true | de |
| eldorado.dnb.zdberstkatid | 2132560-1 |