Nitrooxymethyl substituted analogues of Celecoxib were synthesized and tested for their COX inhibiting, vasodilator, and antiaggregatory activities, as well as for their metabolic stability in human serum and whole blood. The results showed their potency and selectivity in inhibiting the COX isoforms, evaluated in whole human blood, as well as their antiaggregatory activity, to depend closely on the position at which the NO-donor moiety is introduced. All products dilated rat aorta strips precontracted with phenylephrine in a dose dependent manner through a cGMP dependent mechanism. They were stable in human serum while in blood they were metabolically transformed, principally to the related alcohols.

Nitrooxymethyl Substituted Analogues of Celecoxib: Synthesis and Pharmacological Characterization

BOSCHI, Donatella;LAZZARATO, Loretta;ROLANDO, Barbara;FILIERI, Andrea;CENA, Clara;DI STILO, Antonella;FRUTTERO, Roberta;GASCO, Alberto
2009

Abstract

Nitrooxymethyl substituted analogues of Celecoxib were synthesized and tested for their COX inhibiting, vasodilator, and antiaggregatory activities, as well as for their metabolic stability in human serum and whole blood. The results showed their potency and selectivity in inhibiting the COX isoforms, evaluated in whole human blood, as well as their antiaggregatory activity, to depend closely on the position at which the NO-donor moiety is introduced. All products dilated rat aorta strips precontracted with phenylephrine in a dose dependent manner through a cGMP dependent mechanism. They were stable in human serum while in blood they were metabolically transformed, principally to the related alcohols.
CHEMISTRY & BIODIVERSITY
6
3
369
379
http://www3.interscience.wiley.com/journal/122272436/abstract?CRETRY=1&SRETRY=0
Celecoxib analogs; Cyclooxygenase (COX) inhibitors; Vasodilator activity; Anti-aggregatory activity; Inhibitors; Nitric oxide
Donatella Boschi; Loretta Lazzarato; Barbara Rolando; Andrea Filieri; Clara Cena; Antonella Di Stilo; Roberta Fruttero; Alberto Gasco
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/2318/58929
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