Nicorandil analogues containing NO-donor furoxans and related furazans.

Abstract:

: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.

journal_name

Bioorg Med Chem

authors

Boschi D,Cena C,Di Stilo A,Fruttero R,Gasco A

doi

10.1016/s0968-0896(00)00098-5

subject

Has Abstract

pub_date

2000-07-01 00:00:00

pages

1727-32

issue

7

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(00)00098-5

journal_volume

8

pub_type

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