Abstract
Aim: A new series of Quinazoline 4(3H)-one derivative were prepared by reacting quinazoline 4(3H)-one hydrazide with substituted aromatic aldehydes. Quinazoline is used as a potent pharmacological agent with various biological activities such as antimicrobial, antiviral, antitumor, convulsion, anxiety, anti-inflammatory, and analgesic. In this background, we have synthesized a series of Quinazoline 4(3H)-one derivatives (4a-4f) and screened for their anticonvulsant activity. 
 Methods: In this work, Schiff bases were prepared by treating quinazoline 4(3H)-one hydrazide with aromatic aldehydes. Six compounds (4a-4f) were screened for anticonvulsant activity by Isoniazid (INH) and Pentylenetetrazole (PTZ) induced convulsions in mice.
 Results: All the compounds were given satisfactory reaction yields that representing the efficiency of the employed synthetic route. In INH induced convulsion model, delayed the onset of convulsion significantly 4a, 4b, 4d, 4e, 4f when compared to an induction control group. Whereas delayed onset of convulsion was non-significant for 4c. In PTZ induced convulsion model, delayed the onset of convulsion significantly 4a, 4d, 4e, 4f when compared to induction control group. Whereas delayed onset of convulsion was non-significant for 4b and 4c.
 Conclusion: This indicates the anticonvulsant activity to these derivatives which might be due to potentiating GABA activity in the CNS. This anticonvulsant activity was due to presence of electron-donating group like OH, NH2, OCH3 and electron-withdrawing group like CF3 at 2nd and 4th position of aromatic ring attached to hydrazide.
Highlights
Epilepsy is the most common neurological disorder that causes unprovoked, recurrent seizures and affects all ages of people
Whereas delayed onset of convulsion was non-significant for 4b and 4c. This indicates the anticonvulsant activity to these derivatives which might be due to potentiating gamma aminobutyric acid (GABA) activity in the central nervous system (CNS)
This anticonvulsant activity was due to presence of electrondonating group like OH, NH2, OCH3 and electron-withdrawing group like CF3 at 2nd and 4th position of aromatic ring attached to hydrazide
Summary
Epilepsy is the most common neurological disorder that causes unprovoked, recurrent seizures and affects all ages of people. Antiepileptic agents are neither curative nor preventive and are active exclusively as a means of controlling the symptoms of epilepsy. They can directly acts on ion channels or indirectly impact on synthesis, metabolism, or function of neurotransmitters or receptors that control channel opening and closing. Antiepileptic drugs are exhibited their action by various mechanism such as gamma aminobutyric acid (GABA) enhancers, sodium channel blockers, glutamate blockers, calcium channel inhibitors. These drugs are effectively reducing the seizures, whereas their therapeutic efficacy is overcome by some unwanted side effects such as drowsiness, megaloblastic anemia, ataxia, gastrointestinal disturbance, etc. There is an ongoing need to develop more antiepileptic drugs that are effective and endowed with improved safety profiles
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