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

J Bosch; T Roca; J L Catena; O Llorens; J J Pérez; C Lagunas; A G Fernández; I Miquel; A Fernández-Serrat; C Farrerons

doi:10.1016/s0960-894x(00)00329-2

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

Bioorg Med Chem Lett. 2000 Aug 7;10(15):1745-8. doi: 10.1016/s0960-894x(00)00329-2.

Authors

J Bosch¹, T Roca, J L Catena, O Llorens, J J Pérez, C Lagunas, A G Fernández, I Miquel, A Fernández-Serrat, C Farrerons

Affiliation

¹ Laboratory of Organic Chemistry, Faculty of Pharmacy, University of Barcelona, Spain. jbosch@farmacia.far.ub.es

PMID: 10937738
DOI: 10.1016/s0960-894x(00)00329-2

Abstract

The synthesis and structure activity relationships (SAR) of a series of novel selective COX-2 inhibitors are reported. The results show that some of the 1,3,4-triaryl-3-pyrrolin-2-ones 1 are more potent as COX-2 inhibitors than celecoxib, and that lactam Id has the same selectivity.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Cyclooxygenase 2
Cyclooxygenase 2 Inhibitors
Cyclooxygenase Inhibitors / chemical synthesis*
Cyclooxygenase Inhibitors / chemistry
Cyclooxygenase Inhibitors / pharmacology*
Drug Evaluation
Isoenzymes / drug effects
Prostaglandin-Endoperoxide Synthases / drug effects*
Pyrroles / chemical synthesis*
Pyrroles / chemistry
Pyrroles / pharmacology*
Structure-Activity Relationship

Substances

Cyclooxygenase 2 Inhibitors
Cyclooxygenase Inhibitors
Isoenzymes
Pyrroles
Cyclooxygenase 2
Prostaglandin-Endoperoxide Synthases