Medicinal Chemistry

Atta-ur-Rahman  
Honorary Life Fellow
Kings College
University of Cambridge
Cambridge
UK
Email: mc@benthamscience.org

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

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

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.

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

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Article Details

VOLUME: 10
ISSUE: 7
Year: 2014
Page: [711 - 723]
Pages: 13
DOI: 10.2174/1573406409666131128142843
Price: $58