title: Synthesis and biological evaluation of some novel quinoxaline derivatives as anticonvulsant agents.
abstract: In view of their expected anticonvulsant activity, some new derivatives of quinonxaline (V1-7) were designed and synthesized by condensation of different aromatic aldehydes with 2-(2-oxo-3-phenylquinoxalin-1(2H)-yl)acetohydrazide (IV). All synthesized compounds were isolated and confirmed by IR, 1H-NMR, MS, elemental analysis and then tested as anticonvulsant agents. Compound V3 and V1 showed the highest anticonvulsant effect with anticonvulsant potency relative to phenobarbital sodium of 0.8 and 0.75 whereas compound V5 exhibited the lowest relative potency of 0.09. The other compounds showed variable activity between these values as follows: V2 = 0.19, V4 = 0.41, V6 = 0.1 and V7 = 0.15. All compounds showed less activity than the reference compound phenobarbital. But the compounds provided a basis for further optimization.
authors: Department of Pharmaceutical Chemistry, Faculty of Pharmacy (Boys), Al-Azhar University, Cairo, Egypt.
authors: Abdelghany Aly
authors: AA
authors: Elhelby
authors: Rezk Rezk
authors: RR
authors: Ayyad
authors: Mohamed Fathalla
authors: MF
authors: Zayed
mesh_terms: D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis* / Q000494:pharmacology*; D003292:Convulsants; D004305:Dose-Response Relationship, Drug; D007202:Indicators and Reagents; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D013058:Mass Spectrometry; D051379:Mice; D010433:Pentylenetetrazole; D010634:Phenobarbital / Q000627:therapeutic use; D011810:Quinoxalines / Q000138:chemical synthesis* / Q000494:pharmacology*; D012640:Seizures / Q000139:chemically induced / Q000517:prevention & control; D013329:Structure-Activity Relationship
chemical_list: D000927:Anticonvulsants; D003292:Convulsants; D007202:Indicators and Reagents; D011810:Quinoxalines; D010433:Pentylenetetrazole; D010634:Phenobarbital