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Synthesis and Evaluation of Some New (1,2,4) Triazolo(4,3‐a)Quinoxalin‐4(5H)‐one Derivatives as AMPA Receptor Antagonists
Authors:Hamada Abul‐Khair  Salwa Elmeligie  Ashraf Bayoumi  Adel Ghiaty  Ahmed El‐Morsy  Memy H Hassan
Institution:1. Organic Chemistry Department, Faculty of Pharmacy, Al‐Azhar University, , Cairo, Egypt, 11884;2. Organic Chemistry Department, Faculty of Pharmacy, October 6 University, , Sixth of October City, Egypt, 12585;3. Pharmacology and Toxicology Department, Faculty of Pharmacy, Al‐Azhar University, , Cairo, Egypt, 11884
Abstract:This study involves the synthesis and anticonvulsant evaluation of 1‐ethyl‐3‐hydrazinylquinoxaline‐2‐(1H)‐one ( 8 ), its chemical confirmations 9 and 10 and certain (1,2,4) triazolo(4,3‐a)quinoxalin‐4(5H)‐one compounds 11 , 12 , 13 , 13a , 13b , 13c , 13d , 13e , 13f , 14 , 15 , 16 . The structure of the synthesized compounds was confirmed chemically by elemental analyses and spectral data (IR, 1H NMR, 13C NMR, and Mass). Docking studies were preformed to all of the synthesized compounds to predict, in a qualitative way, the anticonvulsant activity of the proposed compounds. There is a promising correlation between the results of molecular modeling and the anticonvulsant activity of the synthesized compounds. The highest fitting value was noticed for compounds 9 and 10 , which showed the highest anticonvulsant activity.
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