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 |
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| Authors: | Biava Mariangela Porretta Giulio C Poce Giovanna Supino Sibilla Manetti Fabrizio Forli Stefano Botta Maurizio Sautebin Lidia Rossi Antonietta Pergola Carlo Ghelardini Carla Norcini Monica Makovec Francesco Giordani Antonio Anzellotti Paola Cirilli Roberto Ferretti Rosella Gallinella Bruno La Torre Francesco Anzini Maurizio Patrignani Paola |
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| Institution: | Dipartimento di Studi di Chimica e Tecnologie del Farmaco, Università La Sapienza, Piazzale Aldo Moro, 5, I-00185 Roma, Italy. |
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| 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. |
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