Potential histamine H2-receptor antagonists: synthesis and pharmacological activity of derivatives containing 3-alkylamino-4-amino-furazan moieties

Giovanni Sorba, Alberto Gasco, Marco Orsetti

Risultato della ricerca: Contributo su rivistaArticolo in rivistapeer review

Abstract

A series of 3-alkylamino-4-(2-((5-dimethylaminomethyl-2-furyl)methylthio)ethylamino)furazans were prepared and tested for their H2-antagonist activities on guinea pig right atrium. A number of differently shaped alkyl substituents on the terminal 3-amino group were favourable for activity. The most potent compound was the cyclohexyl-methyl-substituted derivative (pA2=8.83). Most compounds showed non-competitive antagonism at histamine H1 and muscarinic receptors at concentrations approximately 100 times higher than those producing competitive H2-receptor block. This finding suggests that there is an accessorial binding area on H2-receptor near the site fitted by the diamino-furazan moiety.

Lingua originaleInglese
pagine (da-a)475-478
Numero di pagine4
RivistaEuropean Journal of Medicinal Chemistry
Volume24
Numero di pubblicazione5
DOI
Stato di pubblicazionePubblicato - 1989
Pubblicato esternamente

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