Synthesis and in vitro pharmacology of dimaprit analogues with histamine H2-agonistic and H1-antagonistic activities

Article abstract of DOI:10.1016/0223-5234(96)88284-5

The synthesis and in vitro pharmacology of some dimaprit analogues with histamine H₂-agonistic and additional histamine H₁-antagonistic activities are discussed. 2-Amino-5-(2-aminoethyl)thiazoles can be considered chemically as ring-closed dimaprit analogues, and so the alkylisothiourea structural moiety of dimaprit, S-[3-(N,N-dimethylamino)propyl]isothiourea could replace the propylthiazole or propylimidazole structural moieties of impromidine-like histamine H₂-agonists. The H₂-agonistic activities of a number of N-(3,3-diphenylpropyl)-N'-(ω-isothioureidoalkyl)guanidines indicate that 2-amino-5-(2-aminoethyl)thiazole can indeed be considered as a ring-closed dimaprit analogue.