P. Chaitanya, G. Deepak Reddy, G. Varun, L.M. Srikanth, V.V.S.R. Prasad and A. Ravindernath Pages 711 - 723 ( 13 )
A series of 36 novel substituted quinazolinone derivatives were synthesized and evaluated for their antiinflammatory activity by carrageenan induced paw inflammation model. The ability of these compounds to inhibit cyclooxygenase (COX-1 and 2) enzyme has been determined in-vitro; the results indicated that quinazolinone derivatives were selective towards COX-2 rather than COX-1. Among the quinazolinone derivatives tested, compound 32 showed better inhibition against COX-2 when compared with Celecoxib. Pharmacophore modeling and 3D QSAR studies were performed in order to elucidate structural insights for the anti-inflammatory activity.
Inflammation, COX, quinazolinone, pharmacophore modeling, 3D-QSAR.
Department of Pharmacy and Biotechnology, University College of Technology, Osmania University, Hyderabad, India.