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Design, synthesis, and biological evaluation studies of novel quinazolinone derivatives as anticonvulsant agents |
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| Authors: | Mohamed F. Zayed Hany E. A. Ahmed Abdel-Sattar M. Omar Adel S. Abdelrahim Khaled El-Adl |
| Affiliation: | 1. Pharmaceutical Chemistry Department, College of Pharmacy, Taibah University, Al-madinah Al-munawarah, Kingdom of Saudi Arabia 4. Pharmaceutical Chemistry Department, Faculty of Pharmacy, Al-Azhar University, Cairo, Egypt 5. Organic Chemistry Department, Faculty of Pharmacy, Al-Azhar University, Cairo, Egypt 2. Pharmaceutical Chemistry Department, Faculty of Pharmacy, King AbdulAziz University, Jeddah, Kingdom of Saudi Arabia 3. Pharmaceutical Chemistry Department, Faculty of Pharmacy, Jazan University, Jazan, Kingdom of Saudi Arabia |
| Abstract: | 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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