Synthesis and Biological Evaluation of Quinazolinone Fused Chalcone Derivatives as Anti-inflammatory Agents

Nancy Jain; Nimisha Jain; P K Singour

Nancy Jain Computational and Synthetic Chemistry Division, Department of Pharmaceutical Chemistry, VNS Institute of Pharmacy, Neelbud, Bhopal (M.P.)
Nimisha Jain Computational and Synthetic Chemistry Division, Department of Pharmaceutical Chemistry, VNS Institute of Pharmacy, Neelbud, Bhopal (M.P.)
P K Singour Computational and Synthetic Chemistry Division, Department of Pharmaceutical Chemistry, VNS Institute of Pharmacy, Neelbud, Bhopal (M.P.)

Abstract

In the present study we have designed a new pharmacophore by pharmacophore hybridization approach of drug design. Quinazolinone nucleus has potent anti-inflammatory activities with nearly negligible ulcer index unlike other non steroidal anti-inflammatory drugs. Chalcone also have anti-inflammatory activity. Therefore, here we had tried to synthesize some of the novel quinazolinone fused chalcone derivatives and tested them for their anti-inflammatory activity. The structures of the compound have been confirmed by spectral analysis. Newly synthesized compounds were tested for anti-inflammatory activity using Rat hind paw method. Among the synthesized compounds 3-[1-(3, 4-dimethoxyphenyl)-3-(3-nitrophenyl) allylideneamino]-2-phenylquinazolin-4(3H)-one (4) were found to be most active.

Keywords: Quinazolinone, Schiff base, chalcone, anti-inflammatory activity.