Please use this identifier to cite or link to this item: http://hdl.handle.net/20.500.12779/5464
Title: Synthesis, in vitro, and in vivo biological evaluation and molecular docking simulations of chiral alcohol and ether derivatives of the 1,5-diarylpyrrole scaffold as novel anti-inflammatory and analgesic agents
Authors: Biava, M
PORRETTA G., C
Poce, G
Supino, S
Manetti, Fabrizio 
Forli, S
Botta, Maurizio 
Sautebin, L
Rossi, A
Pergola, C
Ghelardini, C
Norcini, M
Makovec, F
Giordani, A
Anzellotti, P
Cirilli, R
Ferretti, R
Gallinella, B
LA TORRE, F
Anzini, Maurizio 
Patrignani, P.
Issue Date: 2008
Project: None 
Journal: BIOORGANIC & MEDICINAL CHEMISTRY
Abstract: 
Following our previous research on anti-inflammatory drugs (NSAIDs), we report here the synthesis of chiral 1,5-diarylpyrroles derivatives that were characterized for their in vitro inhibitory effects toward cyclooxygenase (COX) isozymes. Analysis of enzymatic affinity and COX-2 selectivity led us to the selection of one compound (+/-)-10b that was further tested in vitro in the human whole blood (HWB) and in vivo for its anti-inflammatory activity in mice. The affinity data have been rationalized through docking simulations.
Description: 
37552
URI: http://hdl.handle.net/20.500.12779/5464
ISSN: 0968-0896
DOI: 10.1016/j.bmc.2008.07.058
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