Terphenyl cyclooxygenase-2 (COX-2) inhibitors: optimization of the central ring and o-biphenyl analogs

…, GC Houghton, RA Copeland, MB Covington…

Index: Pinto, Donald J. P.; Batt, Douglas G.; Pitts, William J.; Petraitis, Joseph J.; Orwat, Michael J.; Wang, Shuaige; Jetter, James W.; Sherk, Susan R.; Houghton, Gregory C.; Copeland, Robert A.; Covington, Maryanne B.; Trzaskos, James M.; Magolda, Ronald L. Bioorganic and Medicinal Chemistry Letters, 1999 , vol. 9, # 7 p. 919 - 924

Full Text: HTML

Citation Number: 21

Abstract

The discovery of terphenyl derivatives as highly selective COX-2 inhibitors resulted from our efforts to overcome poor pharmacokinetics demonstrated by the COX-2 selective diarylthiophene DuP 697 [2-bromo-4-(4′-sulfonylmethyl) phenyl-5-(4′-fluoro) phenylthiophene]. Detailed SAR related to the ortho-biphenyls and variants of the central ring are described herein.