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.
Lingua originale | Inglese |
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pagine (da-a) | 4750-4759 |
Numero di pagine | 10 |
Rivista | Bioorganic and Medicinal Chemistry |
Volume | 13 |
Numero di pubblicazione | 15 |
DOI | |
Stato di pubblicazione | Pubblicato - 1 ago 2005 |
Pubblicato esternamente | Sì |