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NO-donor COX-2 inhibitors. New nitrooxy-substituted 1,5-diarylimidazoles endowed with COX-2 inhibitory and vasodilator properties

Chegaev, K.
Lazzarato, L.
Tosco, P.
Cena, C.
Marini, E.
Rolando, B.
Fruttero, Roberta
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Published in Journal of Medicinal Chemistry. 2007, vol. 50, no. 7, p. 1449-1457
Abstract A series of NO-donor diarylimidazoles derived from the lead compound Cimicoxib were synthesized and evaluated for their COX-2 inhibitory activity and their stability in whole blood as well as for vasodilator properties. The products are partly transformed into the corresponding alcohols following 24-h incubation in whole blood. All of them display good COX-1/COX-2 selectivity, but are less potent than the lead; a molecular modeling study was carried out to investigate their binding mode. The compounds are also capable of relaxing rat aorta strips precontracted with phenylephrine with a NO-dependent mechanism; this property could confer reduced cardiotoxicity with respect to traditional COX-2 inhibitors.
Keywords AnimalsAorta/drug effects/physiologyCyclooxygenase 2 Inhibitors/*chemical synthesis/chemistry/pharmacologyHumansImidazoles/*chemical synthesis/chemistry/pharmacologyModels, MolecularMuscle Contraction/drug effectsMuscle, Smooth, Vascular/drug effects/physiologyNitric Oxide Donors/*chemical synthesis/chemistry/pharmacologyRatsStructure-Activity RelationshipSulfonamides/*chemical synthesis/chemistry/pharmacologyVasodilator Agents/*chemical synthesis/chemistry/pharmacology
Stable URL http://archive-ouverte.unige.ch/unige:10558
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Other version: http://pubs.acs.org/doi/pdfplus/10.1021/jm0607247
PMID: 17335184

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Deposited on : 2010-08-06

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