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

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 1d has the same selectivity.

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Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2000-08, Vol.10 (15), p.1745-1748
Hauptverfasser:	Bosch, Joan, Roca, Tomàs, Catena, Juan-Lorenzo, Llorens, Oriol, Pérez, Juan-Jesús, Lagunas, Carmen, Fernández, Andrés G, Miquel, Ignasi, Fernández-Serrat, Ana, Farrerons, Carles
Format:	Artikel
Sprache:	eng
Schlagworte:	Biological and medical sciences Bones, joints and connective tissue. Antiinflammatory agents Cyclooxygenase 2 Cyclooxygenase 2 Inhibitors Cyclooxygenase Inhibitors - chemical synthesis Cyclooxygenase Inhibitors - chemistry Cyclooxygenase Inhibitors - pharmacology Drug Evaluation Isoenzymes - drug effects Medical sciences Pharmacology. Drug treatments Prostaglandin-Endoperoxide Synthases - drug effects Pyrroles - chemical synthesis Pyrroles - chemistry Pyrroles - pharmacology Structure-Activity Relationship
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Zusammenfassung:	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 1d has the same selectivity.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(00)00329-2