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

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.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Tosco P,Bertinaria M,Di Stilo A,Cena C,Sorba G,Fruttero R,Gasco A

doi

10.1016/j.bmc.2005.05.004

subject

Has Abstract

pub_date

2005-08-01 00:00:00

pages

4750-9

issue

15

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(05)00397-4

journal_volume

13

pub_type

杂志文章

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