Chaitanya P, Reddy G Deepak, Varun G, Srikanth L M, Prasad V V S R, Ravindernath A
Department of Pharmacy and Biotechnology, University College of Technology, Osmania University, Hyderabad, India.
Med Chem. 2014;10(7):711-23. doi: 10.2174/1573406409666131128142843.
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.
合成了一系列36种新型取代喹唑啉酮衍生物，并通过角叉菜胶诱导的爪部炎症模型评估了它们的抗炎活性。已在体外测定了这些化合物抑制环氧化酶（COX-1和COX-2）的能力；结果表明，喹唑啉酮衍生物对COX-2具有选择性，而非COX-1。在所测试的喹唑啉酮衍生物中，与塞来昔布相比，化合物32对COX-2表现出更好的抑制作用。进行了药效团建模和三维定量构效关系研究，以阐明抗炎活性的结构见解。
