Back to Search Start Over

Enhancing the pharmacodynamic profile of a class of selective COX-2 inhibiting nitric oxide donors

Authors :
Carla Ghelardini
Antonio Giordani
Lidia Sautebin
Antonietta Rossi
S. Alfonso
Maurizio Anzini
Claudio Battilocchio
Angela Di Capua
Vincenzo Calderone
Sara Consalvi
Lorenzo Di Cesare Mannelli
Mariangela Biava
Stefano Persiani
Paola Patrignani
Milena Colovic
Melania Dovizio
Giovanna Poce
Alma Martelli
Lara Testai
Biava, M
Battilocchio, C
Poce, G
Alfonso, S
Consalvi, S
Di Capua, A
Calderone, V
Martelli, A
Testai, L
Sautebin, Lidia
Rossi, Antonietta
Ghelardini, C
Di Cesare Mannelli, L
Giordani, A
Persiani, S
Colovic, M
Dovizio, M
Patrignani, P
Anzini, M.
Source :
Bioorganicmedicinal chemistry. 22(2)
Publication Year :
2013

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.

Details

ISSN :
14643391
Volume :
22
Issue :
2
Database :
OpenAIRE
Journal :
Bioorganicmedicinal chemistry
Accession number :
edsair.doi.dedup.....a88d991863c4711b3c08e43ae2ec5f02