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In vivo‐ and in silico‐driven identification of novel synthetic quinoxalines as anticonvulsants and AMPA inhibitors by Hamada S. Abulkhair; Salwa Elmeligie; Adel Ghiaty; Ahmed El‐Morsy; Ashraf H. Bayoumi; Hany E. A. Ahmed; Khaled El‐Adl; Mohamed F. Zayed; Memy H. Hassan; Eman N. Akl; Mona S. El‐Zoghbi is a Chemistry article available to read on EtoBox.
What is In vivo‐ and in silico‐driven identification of novel synthetic quinoxalines as anticonvulsants and AMPA inhibitors about?
The lack of effective therapies for epileptic patients and the potentially harmful consequences of untreated seizure incidents have made epileptic disorders in humans a major health concern. Therefore, new and more potent anticonvulsant drugs are continually sought after, to combat epilepsy. On the basis of the pharmacophoric structural specifications of effective α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) antagonists with an efficient anticonvulsant activity, the present work reports the design and synthesis of two novel sets of quinoxaline derivatives. The anticonvulsant activity of the synthesized compounds was evaluated in vivo according to the pentylenetetrazol-induced seizure protocol, and the results were compared with those of perampanel as a reference drug. Among the synthesized compounds, 24, 28, 32, and 33 showed promising activities with ED values of 37.50, 23.02, 29.16, and 23.86 mg/kg, respectively. Docking studies of these compounds suggested that AMPA binding could be the mechanism of action of these derivatives. Overall, the pharmacophore-based structural optimization, in vivo and in silico docking, and druglikeness studies indicated that the desig
Who reads In vivo‐ and in silico‐driven identification of novel synthetic quinoxalines as anticonvulsants and AMPA inhibitors?
It is typically read by researchers, students, and practitioners in Chemistry.
- Author
- Hamada S. Abulkhair; Salwa Elmeligie; Adel Ghiaty; Ahmed El‐Morsy; Ashraf H. Bayoumi; Hany E. A. Ahmed; Khaled El‐Adl; Mohamed F. Zayed; Memy H. Hassan; Eman N. Akl; Mona S. El‐Zoghbi
- Publisher
- Wiley
- Published
- 2021
- Language
- EN
- Field
- Chemistry (Physical Sciences)