Elz S, Schunack W
Institut für Pharmazie, Johannes Gutenberg-Universität, Mainz.
Arzneimittelforschung. 1988 Jan;38(1):7-10.
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.
在关于类英普咪定组胺H2受体激动剂的构效关系研究中，英普咪定类似胍的合成产生了相应的中间体氰基胍。后者在结构上与西咪替丁相关。因此，对它们在离体豚鼠心房上进行了H2拮抗活性测试。化合物5h被证明比西咪替丁的活性显著更强。具有支链硫醚部分的衍生物没有亲和力。结果与现有的构效关系一致。
