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
Biava, M., Porretta, G.C., Cappelli, A., Vomero, S., Manetti, F., Botta, M., et al. (2005). 1,5-Diarylpyrrole-3-acetic Acids and Esters as Novel Classes of Potent and Highly Selective Cyclooxygenase-2 Inhibitors. JOURNAL OF MEDICINAL CHEMISTRY, 48(9), 3428-3432 [10.1021/jm049121q].
1,5-Diarylpyrrole-3-acetic Acids and Esters as Novel Classes of Potent and Highly Selective Cyclooxygenase-2 Inhibitors
CAPPELLI, ANDREA;MANETTI, FABRIZIO;BOTTA, MAURIZIO;ANZINI, MAURIZIO
2005-01-01
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 siteFile | Dimensione | Formato | |
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https://hdl.handle.net/11365/3017
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