Potential histamine H2-receptor antagonists: synthesis and pharmacological activity of derivatives containing acylamino-furazan moieties.
Analogues of 3-amino-4-[2-[(5-dimethylaminomethyl-2-furyl)methylthio]ethylamino] furazan (1) containing carbonyl groups joined to the amino functions linked to the furazan system have been synthetized and investigated for their H2-antagonist properties on the isolated guinea pig right atrium. The presence of the carbonyl group lowers the activity in respect to the corresponding leads. The decrease in activity is only by 1-2 orders of magnitude in the 3-acylamino-furazan series versus inactivity in the 4-acylamino isomers and in the diacylated series.
Sorba
G
G
Dipartimento die Scienza e Tecnologia del Farmaco-Università di Torino, Italy.
Fruttero
R
R
Di Stilo
A
A
Gasco
A
A
Orsetti
M
M
D000818:Animals; D005663:Furans / Q000138:chemical synthesis* / Q000494:pharmacology; D006168:Guinea Pigs; D006321:Heart / Q000187:drug effects; D006339:Heart Rate / Q000187:drug effects; D006635:Histamine H2 Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology; D066298:In Vitro Techniques
D005663:Furans; D006635:Histamine H2 Antagonists