SYNTHESIS AND IN-VITRO PHARMACOLOGY OF DIMAPRIT ANALOGS WITH HISTAMINE H-2-AGONISTIC AND H-1-ANTAGONISTIC ACTIVITIES

The synthesis and in vitro pharmacology of some dimaprit analogues wit h histamine H-2-agonistic and additional histamine H-2-antagonistic ac tivities are discussed. 2-Amino-5-(2-aminoethyl)thiazoles can be consi dered chemically as ring-closed dimaprit analogues, and so the alkylis othiourea structural moiety of dimaprit, S-[3-(N,N-dimethylamino)propy l]isothiourea could replace the propylthiazole or propylimidazole stru ctural moieties of impromidine-like histamine H-2-agonists. The H-2-ag onistic activities of a number of nylpropyl)-N'-(omega-isothioureidoal kyl)guanidines indicate that 2-amino-5-(2-aminoethyl)thiazole can inde ed be considered as a ring-closed dimaprit analogue.