Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 11, Issue 7, Pages 1197-1205Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/S0968-0896(02)00651-X
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Synthesis and pharmacological characterisation of a series of products obtained by coupling the H-3-antagonist SKF 91486 through appropriate spacers with the NO-donor 3-phenylfuroxan-4-yloxy and 3-benzenesulfonylfuroxan-4-yloxy moieties, as well as with the corresponding furazan substructures, devoid of NO-donating properties, are reported. All the products were tested for their H-3-antagonistic and H-2-agonistic properties on electrically-stimulated guinea-pig ileum segments and guinea-pig papillary muscle, respectively. The whole series of compounds displayed good H-3-antagonist behaviour and feeble partial H-2-agonist activity. Among furoxan derivatives, the benzenesulfonyl hybrid 28, a good NO-donor, triggered a dual NO-dependent muscle relaxation and H3-antagonistic effect on guinea-pig intestine. (C) 2003 Elsevier Science Ltd. All rights reserved.
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