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

Abstract

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.

• Authors: Adel S El-Azab, Kamal E H Eltahir
• Journal: Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 22 Issue 1 Pg. 327-33 (Jan 01 2012) ISSN: 1464-3405 [Electronic] England
• PMID: 22137344 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: Copyright © 2011 Elsevier Ltd. All rights reserved.

Chemical References

• Anticonvulsants
• Quinazolines
• Valproic Acid
• Methaqualone

Topics

• Animals
• Anticonvulsants (pharmacology)
• Chemistry, Pharmaceutical (methods)
• Drug Design
• Humans
• Male
• Methaqualone (pharmacology)
• Mice
• Models, Chemical
• Nervous System (drug effects)
• Quinazolines (pharmacology)
• Seizures (drug therapy)
• Valproic Acid (pharmacology)