Discovery of a potent and selective COX-2 inhibitor in the alkoxy lactone series with optimized metabolic profile

…, N Chauret, DA Nicoll-Griffith, JM Silva, Y Aubin…

文献索引：Leblanc, Yves; Roy, Patrick; Wang, Zhaoyin; Li, Chun Sing; Chauret, Nathalie; Nicoll-Griffith, Deborah A; Silva, Jose M; Aubin, Yves; Yergey, James A; Chan, Chi Chung; Riendeau, Denis; Brideau, Christine; Gordon, Robert; Xu, Lijing; Webb, Janine; Visco, Denise M; Prasit, Petpiboon Bioorganic and medicinal chemistry letters, 2002 , vol. 12, # 22 p. 3317 - 3320

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被引用次数: 13

摘要

The COX-2 inhibitor DFP [5, 5-dimethyl-3-(2-propoxy)-4-methanesulfonylphenyl)-2 (5H)- furanone] was found to have a long half-life in humans. Analogues have been characterized in order to optimize pharmacokinetics. This has lead to the discovery of 5 (S)-(5-ethyl-5- methyl-3-(2-propoxy)-4-methanesulfonylphenyl)-2 (5H)-furanone analogue 11 a potent and selective COX-2 inhibitor which is metabolized to a greater extent than DFP upon ...