Design, synthesis, and biological evaluation studies of novel quinazolinone derivatives as anticonvulsant agents

In view of their expected anticonvulsant activity, some novel derivatives of 6,8-diiodo-2-methyl-3-substituted-quinazolin-4(3H)-ones ( 4 – 14 ) were synthesized, evaluated for their anticonvulsant activity by the maximal electroshock-induced seizure and subcutaneous pentylenetetrazole tests. The neu...

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Veröffentlicht in:Medicinal chemistry research 2013-12, Vol.22 (12), p.5823-5831
Hauptverfasser: Zayed, Mohamed F., Ahmed, Hany E. A., Omar, Abdel-Sattar M., Abdelrahim, Adel S., El-Adl, Khaled
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Sprache:eng
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Zusammenfassung:In view of their expected anticonvulsant activity, some novel derivatives of 6,8-diiodo-2-methyl-3-substituted-quinazolin-4(3H)-ones ( 4 – 14 ) were synthesized, evaluated for their anticonvulsant activity by the maximal electroshock-induced seizure and subcutaneous pentylenetetrazole tests. The neurotoxicity was assessed using rotorod test. All the tested compounds showed considerable anticonvulsant activity in at least one of the anticonvulsant tests. Compounds 5 , 6 , and 8 proved to be the most potent compounds of this series with relatively low neurotoxicity and low toxicity in the median lethal dose test when compared with the reference drugs. The obtained results showed that the most potent compounds could be useful as a template for future design, optimization, and investigation to produce more active analogs.
ISSN:1054-2523
1554-8120
DOI:10.1007/s00044-013-0569-5