Research Articles

2018  |  Vol: 4(5)  |  Issue: 5 (September- October)  |
Design, synthesis and evaluation of novel 2, 3-disubstituted-4-(3H) quinazolinone derivatives

Rakesh Kumar Jain, Varsha Kashaw*

SVN Institute of Pharmaceutical Sciences, Swami Vivekanand University, Sagar (M. P.), India

*Address for Corresponding Author

Dr. (Mrs.) Varsha Kashaw

Prof.  & Head

SVN Institute of Pharmaceutical Sciences,

Swami Vivekanand University Sagar, (M.P.) India


Objective: The aim of the present work was to synthesize some new bioactive 1-(4-substituted-phenyl-3-(4-oxo-2-styryl-4H-quinazolin-3-yl)-urea and to evaluate them for anticonvulsant activity. Materials and methods: A series of novel 2,3 disubstituted-4-(3H)quinazolinone derivatives (RKJ17-48) were synthesized by anthranilic acid using sodium cyanate, substituted anilines and different benzaldehydes. Structures of compounds synthesized were confirmed by IR, 13C NMR and Mass spectroscopic analysis. All synthesized compounds were screened for anti-convulsant activity. The anti-convulsant activity of synthesized compounds was performed against maximal electroshock-induced seizures and PTZ-induced clonic seizures using phenytoin and carbamazepine as standard drug respectively. Same compounds were studied for their Neurotoxicity screens and CNS behavioral activity in mice using rotorod test and actophotometer respectively. Results: Several synthesized compounds have shown anti-convulsant activity as compared to standard drug phenytoin and carbamazepine. Compounds RKJ-46 and RKJ-47 have shown very good anti-convulsant activity. 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 anticonvulsant activity.

Keywords: 4(3H)-Quinazolinones; MES; Pentylenetetrazole, seizure, anticonvulsant

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