Synthesis, structural characterization, and pharmacological profile of a series of Hz-antagonists able to release nitric oxide (NO) are reported. These compounds were obtained by using appropriate spacers to join H-2-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 H-2-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 characterization of new H2-antagonists containing NO-donor moieties, endowed with mixed antisecretory and gastroprotective activities / Bertinaria, M.; Sorba, G.; Medana, C.; Cena, C.; Adami, Maristella; Morini, Giuseppina; Pozzoli, Cristina; Coruzzi, G.; Gasco, A.. - In: HELVETICA CHIMICA ACTA. - ISSN 0018-019X. - 83:(2000), pp. 287-299. [10.1002/(SICI)1522-2675(20000119)83:1<287::AID-HLCA287>3.0.CO;2-2]

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

ADAMI, Maristella;MORINI, Giuseppina;POZZOLI, Cristina;
2000-01-01

Abstract

Synthesis, structural characterization, and pharmacological profile of a series of Hz-antagonists able to release nitric oxide (NO) are reported. These compounds were obtained by using appropriate spacers to join H-2-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 H-2-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.
2000
Synthesis and pharmacological characterization of new H2-antagonists containing NO-donor moieties, endowed with mixed antisecretory and gastroprotective activities / Bertinaria, M.; Sorba, G.; Medana, C.; Cena, C.; Adami, Maristella; Morini, Giuseppina; Pozzoli, Cristina; Coruzzi, G.; Gasco, A.. - In: HELVETICA CHIMICA ACTA. - ISSN 0018-019X. - 83:(2000), pp. 287-299. [10.1002/(SICI)1522-2675(20000119)83:1<287::AID-HLCA287>3.0.CO;2-2]
File in questo prodotto:
File Dimensione Formato  
Prof. Adami Helvetica 2000.pdf

non disponibili

Tipologia: Documento in Post-print
Licenza: NON PUBBLICO - Accesso privato/ristretto
Dimensione 143 kB
Formato Adobe PDF
143 kB Adobe PDF   Visualizza/Apri   Richiedi una copia

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11381/1451745
Citazioni
  • ???jsp.display-item.citation.pmc??? ND
  • Scopus 17
  • ???jsp.display-item.citation.isi??? 15
social impact