Terphenyl cyclooxygenase-2 (COX-2) inhibitors: Optimization of the centralring and o-biphenyl analogs

Authors
Pinto, DJP Batt, DG Pitts, WJ Petraitis, JJ Orwat, MJ Wang, SG Jetter, JW Sherk, SR Houghton, GC Copeland, RA Covington, MB Trzaskos, JM Magolda, RL
Citation
Djp. Pinto et al., Terphenyl cyclooxygenase-2 (COX-2) inhibitors: Optimization of the centralring and o-biphenyl analogs, BIOORG MED, 9(7), 1999, pp. 919-924
Citations number
24
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
9
Issue
7
Year of publication
1999
Pages
919 - 924
Database
ISI
SICI code
0960-894X(19990405)9:7<919:TC(IOO>2.0.ZU;2-1
Abstract
The discovery of terphenyl derivatives as highly selective COX-2 inhibitors resulted from our efforts to overcome poor pharmacokinetics demonstrated b y the COX-2 selective diarylthiophene DuP 697 [2-bromo-4-(4'-sulfonylmethyl )phenyl-5-(4'-fluoro)phenylthiophene]. Detailed SAR related to the ortho-bi phenyls and variants of the central ring are described herein. (C) 1999 DuP ont Pharmaceuticals. Published by Elsevier Science Ltd. All rights reserved .