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  • Title: Design and synthesis of quinazolinone derivatives as anti-inflammatory agents: pharmacophore modeling and 3D QSAR studies.
    Author: Chaitanya P, Reddy GD, Varun G, Srikanth LM, Prasad VV, Ravindernath A.
    Journal: Med Chem; 2014; 10(7):711-23. PubMed ID: 24286396.
    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.
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