[Synthesis and H2-antagonistic action of N,N-substituted 1,3,4-oxadiazole-2,5-diamine. 30. H2-antihistaminics].
The semicarbazides 1 and 5a-c were transformed in high yields into the biureas 3a, b and the thiobiureas 10a-c and 11a-c by addition to appropriate iso(thio)cyanates and subsequently cyclisized to the N,N'-substituted 1,3,4-oxadiazole-2,5-diamines by means of elimination of water or hydrogen sulphide. The synthesized compounds were tested for H2-antagonistic activity at the isolated spontaneously beating guinea-pig atrium, where especially 4a, b and 12c showed pronounced H2-antagonistic action.
D000818:Animals; D055598:Chemical Phenomena; D002621:Chemistry; D003959:Diamines / Q000138:chemical synthesis* / Q000494:pharmacology; D006168:Guinea Pigs; D006321:Heart / Q000187:drug effects; D006635:Histamine H2 Antagonists / Q000138:chemical synthesis*; D066298:In Vitro Techniques; 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 N,N'-substituierter 1,3,4-Oxadiazol-2,5-diamine. 30. Mitteilung: H2-Antihistaminika.