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

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 paren...

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Veröffentlicht in:	European journal of medicinal chemistry 2012-12, Vol.58, p.287-298
Hauptverfasser:	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, Anzini, Maurizio
Format:	Artikel
Sprache:	eng
Schlagworte:	1,5-Diarylpyrroles Acetic Acid Animals Anti-Inflammatory Agents, Non-Steroidal - chemistry Anti-Inflammatory Agents, Non-Steroidal - pharmacokinetics Anti-Inflammatory Agents, Non-Steroidal - pharmacology Biological and medical sciences Carrageenan - antagonists & inhibitors Carrageenan - pharmacology CINODS Constriction, Pathologic - chemically induced Constriction, Pathologic - drug therapy Coxibs Cyclooxygenase 2 - metabolism Cyclooxygenases Dose-Response Relationship, Drug Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacokinetics Enzyme Inhibitors - pharmacology Glycine derivatives Isoenzymes - antagonists & inhibitors Isoenzymes - metabolism Male Medical sciences Mice Miscellaneous Molecular Structure Muscle, Smooth, Vascular - chemistry Muscle, Smooth, Vascular - drug effects Muscle, Smooth, Vascular - metabolism Nitric oxide Nitric Oxide - metabolism Pharmacology. Drug treatments Rats Rats, Sprague-Dawley Rats, Wistar Solubility Structure-Activity Relationship
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Beschreibung
Zusammenfassung:	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. [Display omitted] ► Pharmacodynamic hybrids inhibiting COX-2 isoenzyme. ► Improved solubility due the introduction of an ionisable moiety on the side chain. ► An enhanced nitric oxide releasing profile was highlighted by ex-vivo studies. ► In vivo testing highlighted anti-nociceptive properties for this compounds.
ISSN:	0223-5234 1768-3254
DOI:	10.1016/j.ejmech.2012.10.014