Design and Synthesis of Quinazolinone Derivatives as Anti-inflammatory Agents: Pharmacophore Modeling and 3D QSAR Studies
P. Chaitanya, G. Deepak Reddy, G. Varun, L.M. Srikanth, V.V.S.R. Prasad and A. RavindernathAffiliation:
Department of Pharmacy and Biotechnology, University College of Technology, Osmania University, Hyderabad, India.
AbstractA 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.
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