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

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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
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2014
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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.

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Bioorganic and Medicinal Chemistry

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22

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2

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Medicinal and biomolecular chemistry

Medicinal and biomolecular chemistry not elsewhere classified

Organic chemistry

Pharmacology and pharmaceutical sciences

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