Trumm K A, Sattler H J, Postius S, Szelenyi I, Schunack W
Arzneimittelforschung. 1985;35(3):573-7.
In studies on structure-activity relationships of histamine H2-receptor antagonists, C-2 basically substituted thiazoles were prepared and tested for their H2-antihistaminic activity on the isolated guinea-pig atrium and on the histamine stimulated acid secretion of the anaesthetized rat. As a basic substituent the dimethylaminomethyl group is especially suitable, while cyclic guanidines lead to lower H2-antagonistic activity.
在组胺H2受体拮抗剂的构效关系研究中，制备了C-2位基本取代的噻唑，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抗组胺活性。作为碱性取代基，二甲基氨基甲基特别合适，而环状胍会导致较低的H2拮抗活性。
