Synthesis and biological evaluation of 1,3,4-triaryl-3-pyrrolin-2-ones, a new class of selective cyclooxygenase-2 inhibitors

Authors
Bosch, J Roca, T Catena, JL Llorens, O Perez, JJ Lagunas, C Fernandez, AG Miquel, I Fernandez-Serrat, A Farrerons, C
Citation
J. Bosch et al., Synthesis and biological evaluation of 1,3,4-triaryl-3-pyrrolin-2-ones, a new class of selective cyclooxygenase-2 inhibitors, BIOORG MED, 10(15), 2000, pp. 1745-1748
Citations number
26
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
15
Year of publication
2000
Pages
1745 - 1748
Database
ISI
SICI code
0960-894X(20000807)10:15<1745:SABEO1>2.0.ZU;2-H
Abstract
The synthesis and structure-activity relationships (SAR) of a series of nov el selective COX-2 inhibitors are reported. The results show that some of t he 1,3,4-triaryl-3-pyrrolin-2-ones 1 are more potent as COX-2 inhibitors th an celecoxib, and that lactam 1d has the same selectivity. (C) 2000 Elsevie r Science Ltd. All rights reserved.