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Updated: Aug 12, 2026

Modification and Functionalization of the Guanidine Group by Tailor-made Precursors
Published on: April 27, 2017
H3 receptor ligands: new imidazole H3-antagonists endowed with NO-donor properties
1Dipartimento di Scienza e Tecnologia del Farmaco, Via P Giuria, 9-10125 Turin, Italy. massimo.bertinaria@unito.it
Abstract:
Synthesis and pharmacological properties of a group of compounds obtained by coupling the H(3)-antagonist SKF 91486 with the NO-donor 3-phenylfuroxan-4-yloxy and 3-benzenesulfonylfuroxan-4-yloxy moieties, as well as with the corresponding furazan analogues, devoid of NO-donating properties, are reported. All the products were tested for their H(3)-antagonistic and H(2)-agonistic properties on electrically-simulated guinea-pig ileum segments and guinea-pig papillary muscle, respectively. All the synthesised compounds displayed good H(3)-antagonistic properties (pA(2) range 7.02-8.49) while behaving only as weak partial H(2)-agonists. Derivative 28, the best NO-donor of the series, was able to trigger a dual NO-dependent muscle relaxation and H(3)-antagonistic effect on guinea-pig illeum.
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