Effect of structural modification of enol-carboxamide-type nonsteroidal antiinflammatory drugs on COX-2/COX-1 selectivity

…, R Sorcek, HC Wong, Z Meng, I Potocki…

文献索引：Lazer, Edward S.; Miao, Clara K.; Cywin, Charles L.; Sorcek, Ronald; Wong, Hin-Chor; Meng, Zhaoxing; Potocki, Ian; Hoermann, MaryAnn; Snow, Roger J.; Tschantz, Matt A.; Kelly, Terence A.; McNeil, Daniel W.; Coutts, Simon J.; Churchill, Laurie; Graham, Anne G.; David, Eva; Grob, Peter M.; Engel, Wolfhard; Meier, Hans; Trummlitz, Guenter Journal of Medicinal Chemistry, 1997 , vol. 40, # 6 p. 980 - 989

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被引用次数: 82

摘要

Meloxicam (5), an NSAID in the enol-carboxamide class, was developed on the basis of its antiinflammatory activity and relative safety in animal models. In subsequent screening in microsomal assays using human COX-1 and COX-2, we discovered that it possessed a selectivity profile for COX-2 superior to piroxicam and other marketed NSAIDs. We therefore embarked on a study of enol-carboxamide type compounds to determine if COX-2 ...