1,5-Diarylpyrrole-3-acetic Acids and Esters as Novel Classes of Potent and Highly Selective Cyclooxygenase-2 Inhibitors

A small set of substituted 1,5-diarylpyrrole-3-acetic and -glyoxylic acid derivatives have been synthesized, and their cyclooxygenase (COX-1 and COX-2) inhibiting properties have been evaluated. Some compounds proved to be highly selective COX-2 inhibitors, and their affinity data have been rational...

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Veröffentlicht in:	Journal of medicinal chemistry 2005-05, Vol.48 (9), p.3428-3432
Hauptverfasser:	Biava, Mariangela, Porretta, Giulio Cesare, Cappelli, Andrea, Vomero, Salvatore, Manetti, Fabrizio, Botta, Maurizio, Sautebin, Lidia, Rossi, Antonietta, Makovec, Francesco, Anzini, Maurizio
Format:	Artikel
Sprache:	eng
Schlagworte:	Acetates - chemical synthesis Acetates - chemistry Acetates - pharmacology Animals Binding Sites Biological and medical sciences Bones, joints and connective tissue. Antiinflammatory agents Cell Line Cyclooxygenase 1 Cyclooxygenase 2 Cyclooxygenase 2 Inhibitors Cyclooxygenase Inhibitors - chemical synthesis Cyclooxygenase Inhibitors - chemistry Cyclooxygenase Inhibitors - pharmacology Esters - chemical synthesis Esters - chemistry Esters - pharmacology Medical sciences Membrane Proteins Mice Models, Molecular Pharmacology. Drug treatments Prostaglandin-Endoperoxide Synthases - chemistry Prostaglandin-Endoperoxide Synthases - metabolism Pyrroles - chemical synthesis Pyrroles - chemistry Pyrroles - pharmacology
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Beschreibung
Zusammenfassung:	A small set of substituted 1,5-diarylpyrrole-3-acetic and -glyoxylic acid derivatives have been synthesized, and their cyclooxygenase (COX-1 and COX-2) inhibiting properties have been evaluated. Some compounds proved to be highly selective COX-2 inhibitors, and their affinity data have been rationalized through docking simulations in terms of interactions with a crystallographic model of the COX-2 binding site.
ISSN:	0022-2623 1520-4804
DOI:	10.1021/jm049121q