Design, Synthesis and Anticonvulsant Activity of 2-(2-Phenoxy) phenyl- 1,3,4-oxadiazole Derivatives
| Author | Sayyed Abbas Tabatabai | en |
| Author | Saoka Barghi Lashkari | en |
| Author | Mohammad Reza Zarrindast | en |
| Author | Mohammadreza Gholibeikian | en |
| Author | Abbas Shafiee | en |
| Issued Date | 2013-03-31 | en |
| Abstract | Benzodiazepines are useful drugs for treatment of sleep disorders, anxiety, seizure cases and skeletal muscle cramps. Some derivatives of 2-(2-Phenoxy) phenyl-1, 3, 4-oxadiazole were synthesized as benzodiazepine receptor agonists. Conformational analysis and superimposition of energy minima conformers of the compounds on estazolam, a known benzodiazepine agonist, reveal that the main proposed benzodiazepine pharmacophores were well matched. Anticonvulsant activity of the synthesized compounds, determined by pentylenetetrazole-induced lethal convulsion test, showed that the introduction of an amino substituent in position 5 of 1,3,4- oxadiazole ring generates compound 9 which has a respectable effect. The results are in agreement with SAR of benzodiazepine receptor ligands since the elimination of electronegative substituent in position 2 of phenoxy ring or position 4 of phenyl ring reduces the anticonvulsant activity. | en |
| DOI | https://doi.org/10.22037/ijpr.2013.1277 | en |
| Keyword | 1,3,4-Oxadiazole derivatives | en |
| Keyword | Synthesis | en |
| Keyword | Conformational analysis | en |
| Keyword | Anticonvulsant activity | en |
| Publisher | Brieflands | en |
| Title | Design, Synthesis and Anticonvulsant Activity of 2-(2-Phenoxy) phenyl- 1,3,4-oxadiazole Derivatives | en |
| Type | Original Article | en |
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