Egypt
Research Article
Molecular Docking, Synthesis and Biological Evaluation of Some Novel
2-Substituted-3-allyl-4(3H)-quinazolinone Derivatives as Anticonvulsant
Agents
Author(s): Hamada S Abulkhair, Kamal M El-Gamal, Khaled El-Adl and Mohamed F FadlHamada S Abulkhair, Kamal M El-Gamal, Khaled El-Adl and Mohamed F Fadl
A new series of 2-substituted-3-allyl-4(3H)-quinazolinone derivatives (4a-e-8a-d) were synthesized and evaluated for their anticonvulsant activity against pentylenetetrazole (PTZ)-induced seizures and maximal electroshock test in mice and compared with the reference drugs methaqualone and sodium valproate. The neurotoxicity was assessed using rotarod test. The molecular modeling was performed for all synthesized compounds to predict their binding affinity towards GABA-A receptor as a proposed mode of their anticonvulsant activity. The data obtained from the molecular docking was strongly correlated with that obtained from the biological screening which revealed that; compounds 4c, 4b and 4d showed the highest binding affinities towards GABA-A receptor and also showed the highest anticonvulsant activities in experimental mice with relatively low neurotoxicity and low toxicity in the me.. Read More»
DOI:
10.4172/2161-0444.1000404
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