Synthesis, structural characterization, and pharmacological profile of a series of H2-antagonists able to release nitric oxide (NO) are reported. These compounds were obtained by using appropriate spacers to join H2-antagonistic pharmacophoric groups related to lamtidine and tiotidine to different NO-donor moieties such as esters of HNO3 , nitrosothio groups, and benzenesulfonyl-substituted furoxans. All of the compounds were tested for their NO-donor properties. Furthermore, the hybrid structures synthesized, together with some selected reference compounds, were tested for their H2-antagonistic properties, both in vitro and in vivo, and for their gastroprotective effects. Only the hybrid compounds were able both to antagonize histamine effects on guinea-pig papillary muscle and to display in vivo antisecretory and gastroprotective action. The best results were obtained with the lamtidine/furoxan hybrid structure.

Synthesis and pharmacological characterisation of new H2-antagonists containing NO-donor moieties, endowed with mixed antisecretory and gastroprotective activities.

BERTINARIA, Massimo;SORBA, Giovanni;MEDANA, Claudio;CENA, Clara;GASCO, Alberto
2000

Abstract

Synthesis, structural characterization, and pharmacological profile of a series of H2-antagonists able to release nitric oxide (NO) are reported. These compounds were obtained by using appropriate spacers to join H2-antagonistic pharmacophoric groups related to lamtidine and tiotidine to different NO-donor moieties such as esters of HNO3 , nitrosothio groups, and benzenesulfonyl-substituted furoxans. All of the compounds were tested for their NO-donor properties. Furthermore, the hybrid structures synthesized, together with some selected reference compounds, were tested for their H2-antagonistic properties, both in vitro and in vivo, and for their gastroprotective effects. Only the hybrid compounds were able both to antagonize histamine effects on guinea-pig papillary muscle and to display in vivo antisecretory and gastroprotective action. The best results were obtained with the lamtidine/furoxan hybrid structure.
83
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BERTINARIA M.; SORBA G.; MEDANA C.; C. CENA; ADAMI M.; MORINI G.; POZZOLI C.; CORUZZI G.; GASCO A.
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/2318/1042
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