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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
1 , * 2 , 2 , 3 , 3
1  Department Of Pharmaceutical Chemistry, R.C. Patel Institute of Pharmaceutical Education & Research, Shirpur-425405,Dist. Dhule (MS)
2  Wilson college, Girgaon Chawpatty,Mumbai 400007 , Maharashtra, India
3  Departamento de Química Orgánica, Facultad de Ciencias, Universidad of Santiago De Compostela, Alfonso X el Sabio, Lugo 27002, Spain


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.

Keywords: Dioxoisoindolin-2-yl; Azetidinone; Microwave irradiation; Anticonvulsant evaluation; CNS depression.