[Synthesis and H2-antagonistic action of N3, N5-substituted 1,2, 4-oxadiazole-3, 5-diamine. 26. H2-antihistaminics].
N5-(3-[3-(1-Piperidinylmethyl)phenoxy) phenoxy]propyl)-1,2, 4-oxadiazole-3, 5-diamines and N5(2-[(5-dimethylaminomethyl-2-furanyl) methylthio] ethyl)-1,2,4-oxadiazole-3,5-diamines with different N3-substituents were prepared and tested for their H2-antihistaminic activity on the isolated guinea-pig atrium. They were synthesized by nucleophilic substitution of the appropriate 5-trichloromethyloxadiazoles with the amines 3 and 11. Of the prepared substances 10a,c in particular showed high H2-antagonistic activity.
D000818:Animals; D055598:Chemical Phenomena; D002621:Chemistry; D003959:Diamines / Q000138:chemical synthesis* / Q000494:pharmacology; D006168:Guinea Pigs; D006635:Histamine H2 Antagonists / Q000138:chemical synthesis*; D066298:In Vitro Techniques; D009682:Magnetic Resonance Spectroscopy; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects; D010069:Oxadiazoles / Q000138:chemical synthesis* / Q000494:pharmacology
D003959:Diamines; D006635:Histamine H2 Antagonists; D010069:Oxadiazoles
Synthese und H2-antagonistische Wirkung N3, N5-substituierter 1,2, 4-oxadiazol-3,5-diamine. 26. mitteilung: h2-antihistaminika.