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Merck

Edaravone derivatives containing NO-donor functions.

Journal of medicinal chemistry (2008-12-31)
Konstantin Chegaev, Clara Cena, Marta Giorgis, Barbara Rolando, Paolo Tosco, Massimo Bertinaria, Roberta Fruttero, Pierre-Alain Carrupt, Alberto Gasco
RESUMO

A new series of polyvalent drugs obtained by joining edaravone with NO-donor moieties is described. All compounds display high antioxidant power together with NO-dependent vasodilator properties. The analysis of a number of molecular descriptors shows that the antioxidant activity, which is tightly linked to the presence of the edaravone substructure, is principally modulated by lipophilicity. These products are potentially useful in the treatment of cardiovascular disorders in which EDRF deficiency and ROS excess are involved.

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Sigma-Aldrich
3-Methyl-1-phenyl-2-pyrazoline-5-one, 99%