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Your search keyword '"Consalvi, Sara"' showing total 4 results
Start Over Author "Consalvi, Sara" Topic anti-inflammatory agents
4 results on '"Consalvi, Sara"'

2. Synthesis, biological evaluation and docking analysis of a new series of methylsulfonyl and sulfamoyl acetamides and ethyl acetates as potent COX-2 inhibitors.

Author

Consalvi, Sara, Alfonso, Salvatore, Di Capua, Angela, Poce, Giovanna, Pirolli, Adele, Sabatino, Manuela, Ragno, Rino, Anzini, Maurizio, Sartini, Stefania, La Motta, Concettina, Di Cesare Mannelli, Lorenzo, Ghelardini, Carla, and Biava, Mariangela

Subjects
*SULFONYL compounds, *ACETAMIDE, *ACETATES, *CYCLOOXYGENASE 2 inhibitors, *MOLECULAR docking, *CHEMICAL stability
Abstract

We report herein the synthesis, biological evaluation and docking analysis of a new series of methylsulfonyl, sulfamoyl acetamides and ethyl acetates that selectively inhibit cyclooxygenase-2 (COX-2) isoform. Among the newly synthesized compounds, some of them were endowed with a good activity against COX-2 and a good selectivity COX-2/COX-1 in vitro as well as a desirable analgesic activity in vivo, proving that replacement of the ester moiety with an amide group gave access to more stable derivatives, characterized by a good COX-inhibition. [ABSTRACT FROM AUTHOR]

Published
2015
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3. A class of pyrrole derivatives endowed with analgesic/anti-inflammatory activity.

Author

Battilocchio, Claudio, Poce, Giovanna, Alfonso, Salvatore, Porretta, Giulio Cesare, Consalvi, Sara, Sautebin, Lidia, Pace, Simona, Rossi, Antonietta, Ghelardini, Carla, Di Cesare Mannelli, Lorenzo, Schenone, Silvia, Giordani, Antonio, Di Francesco, Luigia, Patrignani, Paola, and Biava, Mariangela

Subjects
*PYRROLE derivatives, *ANALGESICS, *ANTI-inflammatory agents, *DRUG synthesis, *CYCLOOXYGENASES, *NONSTEROIDAL anti-inflammatory agents, *DINOPROSTONE
Abstract

Abstract: We report the synthesis and bio-pharmacological evaluation of a class of pyrrole derivatives featuring a small appendage fragment (carbaldehyde, oxime, nitrile) on the central core. Compound 1c proved to be extremely effective in vivo, showing an interesting anti-nociceptic profile that is comparable to reference compounds already marketed, hence representing a great stimulus for a further improvement of this class of molecules. [Copyright &y& Elsevier]

Published
2013
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4. Improving the solubility of a new class of antiinflammatory pharmacodynamic hybrids, that release nitric oxide and inhibit cycloxygenase-2 isoenzyme

Author

Biava, Mariangela, Battilocchio, Claudio, Poce, Giovanna, Alfonso, Salvatore, Consalvi, Sara, Porretta, Giulio Cesare, Schenone, Silvia, Calderone, Vincenzo, Martelli, Alma, Testai, Lara, Ghelardini, Carla, Di Cesare Mannelli, Lorenzo, Sautebin, Lidia, Rossi, Antonietta, Giordani, Antonio, Patrignani, Paola, and Anzini, Maurizio

Subjects
*ANTI-inflammatory agents, *SOLUBILITY, *CYCLOOXYGENASES, *PHARMACODYNAMICS, *NITRIC oxide, *ISOENZYMES, *NONSTEROIDAL anti-inflammatory agents
Abstract

Abstract: The development of a novel class of pharmacodynamic hybrids that inhibits COX-2 isoform is reported. These molecules display enhanced nitric oxide releasing properties due to the presence of an ionisable moiety. The in vivo analgesic/anti-inflammatory activity was maintained in relation to the parent compounds. [Copyright &y& Elsevier]

Published
2012
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