European Journal of Medicinal Chemistry p. 673 - 678 (1995)
Update date:2022-07-29
Topics:
Christiaans
Van Der Goot
Menge
Timmerman
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.
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