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.

1,5-Diarylpyrrole-3-acetic Acids and Esters as Novel Classes of Potent and Selective COX-2 Inhibitors, / Biava, Mariangela; Porretta, Giulio Cesare; Cappelli, A; Vomero, S; Botta, M; Manetti, F; Giorni, G; Sautebin, L; Rossi, A; Makovec, F; Anzini, M.. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0022-2623. - STAMPA. - 48:(2005), pp. 3428-3432. [10.1021/jm049121q]

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

BIAVA, Mariangela;PORRETTA, Giulio Cesare;
2005

Abstract

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.
2005
01 Pubblicazione su rivista::01a Articolo in rivista
1,5-Diarylpyrrole-3-acetic Acids and Esters as Novel Classes of Potent and Selective COX-2 Inhibitors, / Biava, Mariangela; Porretta, Giulio Cesare; Cappelli, A; Vomero, S; Botta, M; Manetti, F; Giorni, G; Sautebin, L; Rossi, A; Makovec, F; Anzini, M.. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0022-2623. - STAMPA. - 48:(2005), pp. 3428-3432. [10.1021/jm049121q]
File allegati a questo prodotto
Non ci sono file associati a questo prodotto.

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11573/121309
 Attenzione

Attenzione! I dati visualizzati non sono stati sottoposti a validazione da parte dell'ateneo

Citazioni
  • ???jsp.display-item.citation.pmc??? 0
  • Scopus 55
  • ???jsp.display-item.citation.isi??? 53
social impact