Design and Synthesis of Quinazolinone Derivatives as Anti-inflammatory Agents: Pharmacophore Modeling and 3D QSAR Studies
G. Deepak Reddy,
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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