Buschauer A, Postius S, Szelenyi I, Schunack W
Arzneimittelforschung. 1985;35(7):1025-9.
Starting with isohistamines and their homologues or from appropriately hydrogenated imidazo[1,2-c]pyrimidines, imidazo[1,2-c] [1,3]diazepines and -diazocines, H2-antihistaminics with cyanoguanidine and 2-nitro-1,1-ethenediamine structure were prepared and tested for their H2-antagonistic activity on the isolated guinea-pig atrium and on the histamine-stimulated acid secretion of the anaesthetized rat. While the cyanoguanidines 3a-c,f were weaker in comparison to cimetidine, or inactive, 12a-e,g-l, 17 and 19 possessed markedly stronger activity, whereby the activity reaches a maximal effect at the rat stomach when cyanoguanidine and imidazole ring are connected with a three-membered chain. The activity of the 2-nitro-1,1-ethenediamines 15b,h,l exceed that of the comparable cyanoguanidines at both test models.
从等组胺及其同系物或由适当氢化的咪唑并[1,2 - c]嘧啶、咪唑并[1,2 - c][1,3]二氮杂卓和 - 二氮杂辛开始，制备了具有氰基胍和2 - 硝基 - 1,1 - 乙二胺结构的H2 - 抗组胺药，并在离体豚鼠心房和麻醉大鼠的组胺刺激胃酸分泌实验中测试了它们的H2 - 拮抗活性。与西咪替丁相比，氰基胍3a - c、f的活性较弱或无活性，而12a - e、g - l、17和19具有明显更强的活性，当氰基胍和咪唑环通过三元链连接时，在大鼠胃中活性达到最大效果。在两个测试模型中，2 - 硝基 - 1,1 - 乙二胺15b、h、l的活性均超过了可比的氰基胍。
