title: Nitrooxymethyl-substituted analogues of celecoxib: synthesis and pharmacological characterization.
abstract: Nitrooxymethyl-substituted analogues of celecoxib were synthesized and tested for their cyclooxygenase (COX)-inhibiting, vasodilator, and anti-aggregatory 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 anti-aggregatory 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.
authors.affiliation: Dipartimento di Scienza e Tecnologia del Farmaco, Università degli Studi di Torino, Via Pietro Giuria 9, Turin.
authors.forename: Donatella
authors.initials: D
authors.lastname: Boschi
authors.forename: Loretta
authors.initials: L
authors.lastname: Lazzarato
authors.forename: Barbara
authors.initials: B
authors.lastname: Rolando
authors.forename: Andrea
authors.initials: A
authors.lastname: Filieri
authors.forename: Clara
authors.initials: C
authors.lastname: Cena
authors.forename: Antonella
authors.initials: A
authors.lastname: Di Stilo
authors.forename: Roberta
authors.initials: R
authors.lastname: Fruttero
authors.forename: Alberto
authors.initials: A
authors.lastname: Gasco