Research Articles

2018  |  Vol: 4(5)  |  Issue: 5 (September- October)  |
Design, synthesis and anticonvulsant activity of some new bioactive 1-(4-substituted-phenyl-3-(4-oxo-2-methyl/phenyl-4H-quinazolin-3-yl)-urea

Rakesh Kumar Jain, Varsha Kashaw*

SVN Institute of Pharmaceutical Sciences, Swami Vivekananda University Sagar (Madhya Pradesh), India

*Address for Corresponding Author

Dr. (Mrs.) Varsha Kashaw

Prof. & Head

SVN Institute of Pharmaceutical Sciences,

Swami Vivekananda University Sagar, Madhya Pradesh, India


Objective: The aim of the present work was to synthesize some new bioactive 1-(4-substituted-phenyl-3-(4-oxo-2-methyl/phenyl-4H-quinazolin-3-yl)-urea and to evaluate them for anticonvulsant activity. Materials and methods: Sixteen compounds were synthesized. Their anticonvulsant activity was evaluated from maximal electroshock-induced seizures and PTZ-induced clonic seizures. MES seizures are considered an animal model of human clonic and/or tonic generalized seizures and PTZ-induced clonic seizures are therefore considered a model of myoclonic/generalized absence epilepsy. Using these basic tests, we can identify and differentiate the anticonvulsant pharmacology of novel compounds. Standard drugs used for both the above studies were phenytoin and carbamazepine respectively. All the test compounds were suspended in 0.5% w/v methyl cellulose.  In each of the experiment a control group was made which received the vehicle (0.5% w/v methyl cellulose). Results: Compounds showed significant anticonvulsant activity with low neurotoxicity when compared with the reference drug.Conclusion: Present study explored that substitution of 4(3H)-quinazolinone at second and third position of 4(3H)-quinazolinone leads to the development of new chemical entities with potent sedative-hypnotic as compared to anticonvulsant activity.

Keywords: 4(3H)-Quinazolinone; MES; Subcutaneous pentylenetetrazole induced seizure

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