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  • Title: Non-imidazole histamine NO-donor H3-antagonists.
    Author: Tosco P, Bertinaria M, Di Stilo A, Cena C, Fruttero R, Gasco A.
    Journal: Farmaco; 2005; 60(6-7):507-12. PubMed ID: 15927183.
    Abstract:
    Recently a series of H3-antagonists related to Imoproxifan was realised (I); in these products the oxime substructure of the lead was constrained in NO-donor furoxan systems and in the corresponding furazan derivatives. In this paper, a new series of compounds derived from I by substituting the imidazole ring with the ethoxycarbonylpiperazino moiety present in the non-imidazole H3-ligand A-923 is described. For all the products synthesis and preliminary pharmacological characterisation, as well as their hydrophilic-lipophilic balance, are reported. The imidazole ring replacement generally results in a decreased H3-antagonist activity with respect to the analogues of series I and, in some cases, induces relaxing effects on the electrically contracted guinea-pig ileum, probably due to increased affinity for other receptor systems.
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