Journal
MEDICINAL CHEMISTRY RESEARCH
Volume 22, Issue 12, Pages 5823-5831Publisher
SPRINGER BIRKHAUSER
DOI: 10.1007/s00044-013-0569-5
Keywords
Quinazolin-4(3H)-one; Epilepsy; Neurotoxicity; Synthesis; Anticonvulsant
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Funding
- Deanship of Scientific Research at Taibah University, Al-madinah Al-munawarah, KSA [409/432]
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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.
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