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AFRICAN RESEARCH NEXUS

SHINING A SPOTLIGHT ON AFRICAN RESEARCH

biochemistry, genetics and molecular biology

Synthesis and anticonvulsant evaluation of some new 2,3,8-trisubstituted- 4(3H)-quinazoline derivatives

Bioorganic and Medicinal Chemistry Letters, Volume 22, No. 1, Year 2012

A new series of 2,3,8-trisubstituted-4(3H)-quinazoline derivatives were synthesized, evaluated for their anticonvulsant activity against electrically (MES) and chemically (PTZ, picrotoxin and Strychnine) induced seizures and compared with the standard drugs methaqualone and sodium valproate. Compounds 3, 17 and 22 proved to be the most potent compounds of this series with relatively low neurotoxicity and low toxicity in the median lethal dose test as compared with the reference drugs. The obtained results showed that the most active compounds could be useful as a template for future design, modification and investigation to produce more active analogs. © 2011 Elsevier Ltd. All rights reserved.

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