Synthesis and biological evaluation of some novel quinoxaline derivatives as anticonvulsant agents

Abdelghany Aly Elhelby; Rezk Rezk Ayyad; Mohamed Fathalla Zayed

doi:10.1055/s-0031-1296214

Arzneimittelforschung, Table of Contents

Arzneimittelforschung 2011; 61(7): 379-381
DOI: 10.1055/s-0031-1296214

CNS-active Drugs · Hypnotics · Psychotropics · Sedatives

Editio Cantor Verlag Aulendorf (Germany)

Synthesis and biological evaluation of some novel quinoxaline derivatives as anticonvulsant agents

Abdelghany Aly Elhelby

¹Department of Pharmaceutical Chemistry, Faculty of Pharmacy (Boys), Al-Azhar University, Cairo, Egypt

,

Rezk Rezk Ayyad

¹Department of Pharmaceutical Chemistry, Faculty of Pharmacy (Boys), Al-Azhar University, Cairo, Egypt

,

Mohamed Fathalla Zayed

¹Department of Pharmaceutical Chemistry, Faculty of Pharmacy (Boys), Al-Azhar University, Cairo, Egypt

²Department of Pharmaceutical Chemistry, Faculty of Pharmacy (Boys), Taibah University, Al-Madinah Al-munawarah, Kingdom of Saudi Arabia

› Author Affiliations

Abstract

In view of their expected anticonvulsant activity, some new derivatives of quinon-xaline (V1–7) were designed and synthesized by condensation of different aromatic aldehydes with 2-(2-oxo-3-phenyl-quinoxalin-1 (2H) -yl) acetohydrazide (IV). All synthesized compounds were isolated and confirmed by IR, 1H-NMR, MS, elemental analysis and then tested as anti-convulsant 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.

Key words

Anticonvulsant drugs - Arylidene - Quinoxaline derivatives - Synthesis

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References

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