Bioorganic and Medicinal Chemistry Letters p. 919 - 924 (1999)
Update date:2022-08-03
Topics:
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.
The discovery of terphehyl 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.
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