Herewith, we report the design and synthesis of a series of N-(3-chloro-2-oxo-4-substituted phenyl azetidin-1-yl)-2-(1,3-dioxoisoindolin-2-yl)acetamide 7(a-l) derivatives, obtained by condensation of Schiff’s base and chloroacetyl chloride in dimethyl formamide as solvent and few drops of triethyl amine as a catalyst under microwave irradiation for about 3-4 min (700 W) at 800C based on four component pharmacophoric model to get structural prerequisite indispensable for anticonvulsant activity. The synthesized derivatives were investigated for CNS depressant, maximal electroshock seizure (MES), subcutaneous pentylenetetrazole (sc-PTZ) induced seizure and neurotoxicity screening. Most of the compounds were found to be potent in MES model. The anticonvulsant screening data shows that 65% of the compounds were found to be active against MES model when compared to 35% sc-PTZ model.
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Microwave-Assisted Facile Synthesis and anticonvulsant evaluation of Novel N-(3-chloro-2-oxo-4-substituted phenyl azetidin-1-yl)-2-(1, 3-dioxoisoindolin-2-yl) acetamides
Published:
03 November 2017
by MDPI
in The 21st International Electronic Conference on Synthetic Organic Chemistry
session Symposium on Microwave Assisted Synthesis
Abstract:
Keywords: Dioxoisoindolin-2-yl; Azetidinone; Microwave irradiation; Anticonvulsant evaluation; CNS depression.