Abstract
Because in some alkylenediisothioureas replacement of one of the isothiourea groups by a guanidino group resulted in a strong increase in agonistic histamine H2-activity, while replacement of the guanidino group of a potent analogue of impromidine by an isothiourea group resulted in a complete loss of histamine H2-activity, it was concluded that guanidino and isothiourea groups are not bio-isosteric for the H2-receptor.
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Sterk, G.J., van der Goot, H. & Timmerman, H. The influence of guanidino and isothiourea groups in histaminergic compounds on H2-activity. Agents and Actions 18, 137–140 (1986). https://doi.org/10.1007/BF01988004
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DOI: https://doi.org/10.1007/BF01988004