Abstract

SYNTHESIS, CHARACTERIZATION AND PHARMACOLOGICAL EVALUATIONS OF SUBSTITUTED QUINAZOLIN-4-(3H)-ONE DERIVATIVE AS NOVEL ANTICONVULSANT AGENTS

Meenu Chaudhary*, Praveen Chaudhary

ABSTRACT

Purpose: To synthesize and evaluate the anticonvulsant activity of substituted Quinazolin-4(3H)-one derivative. Methods: In the present study, total 19 derivatives of two series of substituted Quinazolin-4(3H)-one have been synthesized and elucidated on the basis of analytical and spectral studies such as IR, 1HNMR, and Mass spectroscopy. The preliminary evaluation of these 19 compounds for anti-inflammatory, anticonvulsant, diuretic, antihypertensive and antitubercular activities indicated some of them exhibit moderate to significant activity compared to control group. Further, on the basis of their SAR studies, it has been revealed that substitution at 2, 3 position of Quinazolin-4(3H)-one derivatives may confer various pharmacological activities such as antitumor, anti-HIV, anti-inflammatory, antibacterial and antidepressant etc. Result: out of nineteen synthesized compounds, only four synthesized compounds KA-3, KB-2, KD-1 and IA-1 have shown significant anticonvulsant activity with 90% recovery against MES-induced convulsions acting as GABAA receptor agonist. Conclusion: Among these four compounds, KD-1 and IA-1 has shown most and equieffective activity comparable to standard drug Phenytoin.

Keywords: Quinazolin-4-(3H)-one derivative, SAR study, MES, anticonvulsant activity.