Chemistry and pharmacokinetics of diarylthiophenes and terphenyls as selective COX-2 inhibitors

…, RA Copeland, MB Covington, WJ Pitts, DG Batt…

文献索引：Pinto, Donald J.P.; Copeland, Robert A.; Covington, Maryanne B.; Pitts, William J.; Batt, Douglas G.; Orwat, Michael J.; Lam, Gilbert N.; Joshi, Amita; Chan, Yuk-Charn; Wang, Shuaige; Trzaskos, James M.; Magolda, Ronald L.; Kornhauser, David M. Bioorganic and Medicinal Chemistry Letters, 1996 , vol. 6, # 24 p. 2907 - 2912

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被引用次数: 37

摘要

DuP697, 2-bromo-4-(4′-sulfonylmethyl) phenyl-5-(4′-fluoro) phenylthiophene, is a selective type 2 cyclooxygenase (COX-2) inhibitor. Its relatively weak COX-2 selectivity coupled with a poor human pharmacokinetic profile led us to seek improvements on the in vitro selectivity while at the same time, addressing some of its pharmacokinetic liabilities. In this paper we discuss some strategies at solving the PK issue within a class of COX-2 ...