title: Potential histamine H2-receptor antagonists. Synthesis, conformational studies and activity of novel 3-oxo-1,2,5-thiadiazole 1,1-dioxide derivatives.
abstract: New histamine H2-receptor antagonists bearing a novel "urea equivalent", the 3-oxo-1,2,5-thiadiazole 1,1-dioxide ring, have been synthesized in a transamination reaction. Open chain derivatives have also been obtained. Theoretical conformational analysis of the compounds has been carried out using a molecular modelling program. Semiempirical CNDO/2 calculations have also been performed. The antisecretory and cytoprotective activities of the compounds have been evaluated.
authors.affiliation: Instituto de Química Médica (CSIC), Madrid, Spain.
authors.forename: V J
authors.initials: VJ
authors.lastname: Arán
authors.forename: E
authors.initials: E
authors.lastname: Dávila
authors.forename: M
authors.initials: M
authors.lastname: Francés
authors.forename: P
authors.initials: P
authors.lastname: Goya
authors.forename: J
authors.initials: J
authors.lastname: Gras
authors.forename: A
authors.initials: A
authors.lastname: Martínez
authors.forename: N
authors.initials: N
authors.lastname: Mylonakis
authors.forename: I
authors.initials: I
authors.lastname: Pardo
mesh_terms: D000818:Animals; D000897:Anti-Ulcer Agents / Q000138:chemical synthesis; D002470:Cell Survival / Q000187:drug effects; D006635:Histamine H2 Antagonists / Q000138:chemical synthesis* / Q000737:chemistry; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D008958:Models, Molecular; D008968:Molecular Conformation; D011708:Pylorus / Q000502:physiology; D051381:Rats; D011919:Rats, Inbred Strains; D013830:Thiadiazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
chemical_list: D000897:Anti-Ulcer Agents; D006635:Histamine H2 Antagonists; D013830:Thiadiazoles