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

Massimo Bertinaria, Giovanni Sorba, Claudio Medana, Clara Cena, Maristella Adami, Giuseppina Morini, Cristina Pozzoli, Gabriella Coruzzi, Alberto Gasco

Risultato della ricerca: Contributo su rivistaArticolo in rivistapeer review

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.

Lingua originaleInglese
pagine (da-a)287-299
Numero di pagine13
RivistaHelvetica Chimica Acta
Volume83
Numero di pubblicazione1
DOI
Stato di pubblicazionePubblicato - 2000
Pubblicato esternamente

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