Terphenyl cyclooxygenase-2 (COX-2) inhibitors: Optimization of the central ring and o-biphenyl analogs
摘要:
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. (C) 1999 DuPont Pharmaceuticals. Published by Elsevier Science Ltd. All rights reserved.
Terphenyl cyclooxygenase-2 (COX-2) inhibitors: Optimization of the central ring and o-biphenyl analogs
摘要:
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. (C) 1999 DuPont Pharmaceuticals. Published by Elsevier Science Ltd. All rights reserved.
Terphenyl cyclooxygenase-2 (COX-2) inhibitors: Optimization of the central ring and o-biphenyl analogs
作者:Donald J.P. Pinto、Douglas G. Batt、William J. Pitts、Joseph J. Petraitis、Michael J. Orwat、Shuaige Wang、James W. Jetter、Susan R. Sherk、Gregory C. Houghton、Robert A. Copeland、Maryanne B. Covington、James M. Trzaskos、Ronald L. Magolda
DOI:10.1016/s0960-894x(99)00105-5
日期:1999.4
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. (C) 1999 DuPont Pharmaceuticals. Published by Elsevier Science Ltd. All rights reserved.