Design, synthesis and anticonvulsant activity of 2-[2-Phenoxy] phenyl-1,3,4-oxadiazole derivatives
IJPR-Iranian Journal of Pharmaceutical Research. 2013; 12 (Supp. 1): 105-111
in English
| IMEMR
| ID: emr-193179
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, and 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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Index:
IMEMR (Eastern Mediterranean)
Language:
English
Journal:
Iran. J. Pharm. Res.
Year:
2013
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