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Title

DESIGN, SYNTHESIS AND ANTICONVULSANT ACTIVITY OF 2- (2-PHENOXY) PHENYL- 1, 3, 4-OXADIAZOLE DERIVATIVES

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 Start Page 105 | End Page 111

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.

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