Selective cyclooxygenase-2 inhibitors: heteroaryl modified 1, 2-diarylimidazoles are potent, orally active antiinflammatory agents

…, WE Perkins, K Seibert, AW Veenhuizen…

文献索引：Khanna; Yu; Huff; Weier; Xu; Koszyk; Collins; Cogburn; Isakson; Koboldt; Masferrer; Perkins; Seibert; Veenhuizen; Yuan; Yang; Zhang Journal of Medicinal Chemistry, 2000 , vol. 43, # 16 p. 3168 - 3185

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被引用次数: 105

摘要

A series of heteroaryl modified 1, 2-diarylimidazoles has been synthesized and found to be potent and highly selective (1000-9000-fold) inhibitors of the human COX-2. 3-Pyridyl derived COX-2 selective inhibitor (25) exhibited excellent activity in acute (carrageenan induced paw edema, ED50= 5.4 mg/kg) and chronic (adjuvant induced arthritis, ED50= 0.25 mg/kg) models of inflammation. The relatively long half-life of 25 in rat and dog prompted ...