Literature DB >> 21899204

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

Abdelghany Aly Elhelby1, Rezk Rezk Ayyad, Mohamed Fathalla Zayed.   

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.

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Year:  2011        PMID: 21899204     DOI: 10.1055/s-0031-1296214

Source DB:  PubMed          Journal:  Arzneimittelforschung        ISSN: 0004-4172


  4 in total

1.  A novel method for heterocyclic amide-thioamide transformations.

Authors:  Walid Fathalla; Ibrahim A I Ali; Pavel Pazdera
Journal:  Beilstein J Org Chem       Date:  2017-01-26       Impact factor: 2.883

2.  Synthesis, Modelling, and Anticonvulsant Studies of New Quinazolines Showing Three Highly Active Compounds with Low Toxicity and High Affinity to the GABA-A Receptor.

Authors:  Mohamed F Zayed; Saleh K Ihmaid; Hany E A Ahmed; Khaled El-Adl; Ahmed M Asiri; Abdelsattar M Omar
Journal:  Molecules       Date:  2017-01-24       Impact factor: 4.411

3.  An efficient synthesis of 4-phenoxy-quinazoline, 2-phenoxy-quinoxaline, and 2-phenoxy-pyridine derivatives using aryne chemistry.

Authors:  Mahesh K Zilla; Sheena Mahajan; Rajni Khajuria; Vivek K Gupta; Kamal K Kapoor; Asif Ali
Journal:  RSC Adv       Date:  2021-01-15       Impact factor: 3.361

Review 4.  Recent advances in the transition-metal-free synthesis of quinoxalines.

Authors:  Biplob Borah; L Raju Chowhan
Journal:  RSC Adv       Date:  2021-11-19       Impact factor: 4.036

  4 in total

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