Design and Synthesis of Quinazolinone Derivatives as Anti-inflammatory Agents: Pharmacophore Modeling and 3D QSAR Studies

Title:Design and Synthesis of Quinazolinone Derivatives as Anti-inflammatory Agents: Pharmacophore Modeling and 3D QSAR Studies

Volume: 10 Issue: 7

Author(s): P. Chaitanya, G. Deepak Reddy, G. Varun, L.M. Srikanth, V.V.S.R. Prasad and A. Ravindernath

Affiliation:

Keywords: Inflammation, COX, quinazolinone, pharmacophore modeling, 3D-QSAR.

Abstract: 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.

Cite this article as:

Chaitanya P., Reddy Deepak G., Varun G., Srikanth L.M., Prasad V.V.S.R. and Ravindernath A., Design and Synthesis of Quinazolinone Derivatives as Anti-inflammatory Agents: Pharmacophore Modeling and 3D QSAR Studies, Medicinal Chemistry 2014; 10 (7) . https://dx.doi.org/10.2174/1573406409666131128142843