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Title: Novel Ester and Acid Derivatives of the 1,5-Diarylpyrrole Scaffold as Anti-inflammatory and Analgesic Agents. Synthesis, in vitro and in vivo Biological Evaluation.
Authors: M., Biava
G. C., Porretta
G., Poce
C., Battilocchio
Manetti, Fabrizio 
Botta, Maurizio 
S., Forli
L., Sautebin
A., Rossi
C., Pergola
C., Ghelardini
N., Galeotti
F., Makovec
A., Giordani
P., Anzellotti
P., Patrignani
Anzini, Maurizio 
Issue Date: 2010
Project: None 
A new generation of selective cyclooxygenase-2 (COX-2) inhibitors (coxibs) was developed to circumvent the major side effects of cyclooxygenase-1 (COX-1) and COX-2 inhibitors (stomach ulceration and nephrotoxicity). As a consequence, coxibs are extremely valuable in treating acute and chronic inflammatory conditions. However, the use of coxibs, such as rofecoxib (Vioxx), was discontinued because of the high risk of cardiovascular adverse events. More recent clinical findings highlighted how the cardiovascular toxicity of coxibs could be mitigated by an appropriate COX-1 versus COX-2 selectivity. We previously reported a set of substituted 1,5-diarylpyrrole derivatives, selective for COX-2. Here, we describe the synthesis of new 1,5-diarylpyrroles along with their inhibitory effects in vitro, ex vivo, and in vivo toward COX isoenzymes and their analgesic activity. Isopropyl-2-methyl-5-[4-(methylsulfonyl)phenyl]-1-phenyl-1H-pyrrole-3-acetate (10a), a representative member of the series, was selected for pharmacokinetic and metabolic studies.
ISSN: 0022-2623
DOI: 10.1021/jm901269y
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