[H2-antagonistic activity of the impromidine analog, cyanoguanidine. 37. H2 antihistaminics]

Abstract

In studies on structure-activity relationships among impromidine-like histamine H2-receptor agonists, the synthesis of impromidine analogous guanidines led to the corresponding intermediate cyanoguanidines. The latter are structurally related to cimetidine. For that reason they were tested for H2-antagonistic activity on the isolated guinea-pig atrium. Compound 5h proved to be significantly more potent than cimetidine. Derivatives with branched thioether moiety were devoid of affinity. The results are consistent with existing structure-activity relationships.