SYNTHESIS AND ANTIANXIETY ACTIVITY OF 2-ARYL-3-INDOLACETAMIDE DERIVATIVES

AIM To search for antianxiety drugs with fewer side effects and improved activities. METHODS Reaction of aryl compounds with succinic anhydride to give benzoylpropionic acid. Then, the benzoylpropionic acid was converted to its mixed anhydride with ethyl chloroformate, and the intermediate reacted with the amine of choice to afford the corresponding amide. The amide was reacted with the appropriate phenylhydrazine and anhydrous zinc chloride. A series of 2-aryl-3-indolacetamides derivatives with different substituted groups in their phenyl rings and indole groups were synthesized. RESULTS Twenty new compounds have been synthesized. Their structures were confirmed by IR, ¹HNMR, MS and elemental analysis. The antianxiety activities were screened. The structure activity ralationship has been studied. CONCLUSION Most of the compounds was shown to bind to peripheral benzodiazepine receptor with high affinity. Several compounds exihbited marked antianxiety effects in animal experiments without seizure effects.