EventsThe 21st International Electronic Conference on Synthetic Organic Chemistry
Published
This submission belongs to the session C. Symposium on Microwave Assisted Synthesis of the event The 21st International Electronic Conference on Synthetic Organic Chemistry
Published date
03 Nov, 2017
Citation
Anna Pratima Nikalje, Julio A Seijas Vázquez, M. Pilar Vazquez-Tato, Shailee Tiwari, Mangesh S Ghodke, 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, in Proceedings of The 21st International Electronic Conference on Synthetic Organic Chemistry, 1 November–30 November 2017, MDPI: Basel, Switzerland, doi: 10.3390/ecsoc-21-04810
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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

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Julio A Seijas Vázquez 3
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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
Abstract

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.
Manuscript
Poster
Presentation.pdf
Ultrasound assisted synthesis of 4-(benzyloxy)-N-(3-chloro-2-(substituted phenyl)-4-oxoazetidin-1-yl) benzamide
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