Abstract
AbstractS,S'‐Alkylenediisothioureas were found to show only weak agonistic or antagonistic H2‐activity, depending on the length of the alkylene chain.Introduction of a substituent in the amidino parts of both isothiourea groups resulted in a complete loss of the agonistic activity; only inactive compounds or weakly active H2‐antagonists were obtained.Replacing one of the isothiourea groups of the alkylenediisothioureas with n = 2, 3 or 4 by a guanidino group has hardly any or no effect at all on the histamine H2‐activity on the guinea‐pig right atrium. However, extending the alkylene chain of these guanidylalkylisothioureas to n = 5 and 6 results in a strong increase in the H2‐agonistic activity.
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