TY - JOUR
T1 - Synthesis and pharmacological characterization of new H2-antagonists containing NO-donor moieties, endowed with mixed antisecretory and gastroprotective activities
AU - Bertinaria, Massimo
AU - Sorba, Giovanni
AU - Medana, Claudio
AU - Cena, Clara
AU - Adami, Maristella
AU - Morini, Giuseppina
AU - Pozzoli, Cristina
AU - Coruzzi, Gabriella
AU - Gasco, Alberto
PY - 2000
Y1 - 2000
N2 - 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.
AB - 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.
UR - http://www.scopus.com/inward/record.url?scp=0033966035&partnerID=8YFLogxK
U2 - 10.1002/(SICI)1522-2675(20000119)83:1<287::AID-HLCA287>3.0.CO;2-2
DO - 10.1002/(SICI)1522-2675(20000119)83:1<287::AID-HLCA287>3.0.CO;2-2
M3 - Article
SN - 0018-019X
VL - 83
SP - 287
EP - 299
JO - Helvetica Chimica Acta
JF - Helvetica Chimica Acta
IS - 1
ER -