Autor(en): | Faizi, Mehrdad Jahani, Reza Ebadi, Seyed Abbas Tabatabai, Sayyed Abbas Rezaee, Elham Lotfaliei, Mehrnaz Amini, Mohsen Almasirad, Ali |
Titel: | Novel 4-thiazolidinone derivatives as agonists of benzodiazepine receptors |
Sonstige Titel: | Design, synthesis and pharmacological evaluation |
Sprache (ISO): | en |
Zusammenfassung: | 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. |
Schlagwörter: | benzodiazepine sedative-hypnotic anticonvulsant 4-thiazolidinone derivatives synthesis |
URI: | http://hdl.handle.net/2003/35950 http://dx.doi.org/10.17877/DE290R-17973 |
Erscheinungsdatum: | 2017-01-13 |
Rechte (Link): | http://creativecommons.org/licenses/by/4.0/ |
Enthalten in den Sammlungen: | Original Articles |
Dateien zu dieser Ressource:
Datei | Beschreibung | Größe | Format | |
---|---|---|---|---|
Almasirad_13012017_proof.pdf | DNB | 185.1 kB | Adobe PDF | Öffnen/Anzeigen |
Diese Ressource ist urheberrechtlich geschützt. |
Diese Ressource wurde unter folgender Copyright-Bestimmung veröffentlicht: Lizenz von Creative Commons