title: Design, Synthesis and Anticonvulsant Activity of 2-(2-Phenoxy) phenyl- 1,3,4-oxadiazole Derivatives.
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.
authors.affiliation: Department of Medicinal Chemisty School of Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Iran. ; Phytochemistry Research Center, Shahid Beheshti University of Medical Sciences, Tehran, Iran.
authors.forename: Sayyed Abbas
authors.initials: SA
authors.lastname: Tabatabai
authors.forename: Saoka
authors.initials: S
authors.lastname: Barghi Lashkari
authors.forename: Mohammad Reza
authors.initials: MR
authors.lastname: Zarrindast
authors.forename: Mohammadreza
authors.initials: M
authors.lastname: Gholibeikian
authors.forename: Abbas
authors.initials: A
authors.lastname: Shafiee
keywords: 1,3,4-Oxadiazole derivatives; Anticonvulsant activity; Conformational analysis; Synthesis