Boschi D, Cena C, Di Stilo A, Fruttero R, Gasco A
Dipartimento di Scienze Chimiche, Alimentari, Farmaceutiche, Farmacologiche, Novara, Italy.
Bioorg Med Chem. 2000 Jul;8(7):1727-32. doi: 10.1016/s0968-0896(00)00098-5.
The synthesis and in vitro vasodilating properties of hybrid compounds in which furoxan (1,2,5-oxadiazole 2-oxide) moieties, endowed with different NO-donor properties, were substituted for the nitroxy function of Nicorandil are reported. The corresponding cyanoguanidine analogues are also considered. This approach has led to a series of vasorelaxing compounds devoid of affinity for K(ATP) channels, whose activity is prevalently due to their ability to activate sGC, at the concentrations of the experiments. Related furazan (1,2,5-oxadiazole) derivatives, unable to release nitric oxide were also prepared and studied for control. The amide analogues of Nicorandil display feeble vasorelaxing action not involving the activation of K+ channels, while in the guanidine analogues, this mechanism seems to underlie this action.
