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

Authors :: 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
Source :: Bioorganic & medicinal chemistry [Bioorg Med Chem] 2014 Jan 15; Vol. 22 (2), pp. 772-86. Date of Electronic Publication: 2013 Dec 18.
Publication Year :: 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.<br /> (Copyright © 2013 Elsevier Ltd. All rights reserved.)

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