We report herein the development, synthesis, physicochemical and pharmacological characterization of a novel class of pharmacodynamic hybrids that selectively inhibit cyclooxygenase-2 (COX-2) isoform and present suitable nitric oxide releasing properties. The replacement of the ester moiety with the amide group gave access to in vivo more stable and active derivatives that highlighted outstanding pharmacological properties. In particular, the glycine derivative proved to be extremely active in suppressing hyperalgesia and edema. © 2013 Elsevier Ltd. All rights reserved.
Enhancing the pharmacodynamic profile of a class of selective COX-2 inhibiting nitric oxide donors / Biava, Mariangela; Battilocchio, Claudio; Poce, Giovanna; Alfonso, Salvatore; Consalvi, Sara; Angela Di, Capua; Vincenzo, Calderone; Alma, Martelli; Lara, Testai; Lidia, Sautebin; Antonietta, Rossi; Carla, Ghelardini; Lorenzo Di Cesare, Mannelli; Antonio, Giordani; Stefano, Persiani; Milena, Colovic; Melania, Dovizio; Paola, Patrignani; Maurizio, Anzini. - In: BIOORGANIC & MEDICINAL CHEMISTRY. - ISSN 0968-0896. - STAMPA. - 22:2(2014), pp. 772-786. [10.1016/j.bmc.2013.12.008]
Enhancing the pharmacodynamic profile of a class of selective COX-2 inhibiting nitric oxide donors
BIAVA, Mariangela;BATTILOCCHIO, CLAUDIO;POCE, Giovanna;ALFONSO, SALVATORE;CONSALVI, SARA;
2014
Abstract
We report herein the development, synthesis, physicochemical and pharmacological characterization of a novel class of pharmacodynamic hybrids that selectively inhibit cyclooxygenase-2 (COX-2) isoform and present suitable nitric oxide releasing properties. The replacement of the ester moiety with the amide group gave access to in vivo more stable and active derivatives that highlighted outstanding pharmacological properties. In particular, the glycine derivative proved to be extremely active in suppressing hyperalgesia and edema. © 2013 Elsevier Ltd. All rights reserved.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
