Enhancing the pharmacodynamic profile of a class of selective COX-2 inhibiting nitric oxide donors
Author(s)
Biava, M
Battilocchio, C
Poce, G
Alfonso, S
Consalvi, S
Di Capua, A
Calderone, V
Martelli, A
Testai, L
Sautebin, L
Rossi, A
Ghelardini, C
Di Cesare Mannelli, L
Giordani, A
Persiani, S
Colovic, M
Dovizio, M
Patrignani, P
Anzini, M
Griffith University Author(s)
Year published
2014
Metadata
Show full item recordAbstract
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.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.
View less >
View less >
Journal Title
Bioorganic and Medicinal Chemistry
Volume
22
Issue
2
Subject
Medicinal and biomolecular chemistry
Medicinal and biomolecular chemistry not elsewhere classified
Organic chemistry
Pharmacology and pharmaceutical sciences