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. 2005 Aug 1;13(15):4750-9.
doi: 10.1016/j.bmc.2005.05.004.

Furoxan analogues of the histamine H3-receptor antagonist imoproxifan and related furazan derivatives

Paolo Tosco  1 , Massimo Bertinaria, Antonella Di Stilo, Clara Cena, Giovanni Sorba, Roberta Fruttero, Alberto Gasco
Affiliations

Furoxan analogues of the histamine H3-receptor antagonist imoproxifan and related furazan derivatives

Paolo Tosco et al. Bioorg Med Chem. .

Abstract

Synthesis and pharmacological characterisation of a series of compounds in which the oxime substructure present in imoproxifan was constrained in the pentatomic NO-donor furoxan ring, as well as their structurally related furazan analogues devoid of NO-donating properties, are described. The whole series of products displayed reversible histamine H3-antagonistic activity on guinea-pig ileum. 4-(4-(3-(1H-Imidazol-4-yl)propoxy)phenyl)furoxan-3-carbonitrile 16 was also able to induce partial relaxation when added to the bath after electrical contraction of the guinea-pig ileum during the study of its H3-antagonistic properties. This phenomenon seems to be dependent on NO-mediated sGC activation. The lipophilic-hydrophilic balance of all the products was investigated.

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