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

ISSN: 1875-6638 (Online)
ISSN: 1573-4064 (Print)


Volume 10, 8 Issues, 2014


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Medicinal Chemistry

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Editor-in-Chief:
Atta-ur-Rahman, FRS
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. Rajendra Prasad and A. Ravinder Nath

Affiliation: Department of Chemistry, University College of Technology, Osmania University, Hyderabad, India

Abstract

A series of 36 novel substituted quinazolinone derivatives were synthesized and evaluated for their anti-inflammatory activity by carrageenan induced paw inflammation model. The ability of these compounds to inhibit cyclooxygenase (COX-1 and 2) enzyme has been determined and the results have indicated selectivity towards COX-2 rather than COX-1. Among the quinazolinone derivatives tested, compound 32 was shown for its 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: 9
First Page: 1
Last Page: 13
Page Count: 13
DOI: 10.2174/1573406409666131128142843
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