Potential histamine H2-receptor antagonists. Synthesis, conformational studies and activity of novel 3-oxo-1,2,5-thiadiazole 1,1-dioxide derivatives.
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.
Arán
V J
VJ
Instituto de Química Médica (CSIC), Madrid, Spain.
Dávila
E
E
Francés
M
M
Goya
P
P
Gras
J
J
Martínez
A
A
Mylonakis
N
N
Pardo
I
I
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
D000897:Anti-Ulcer Agents; D006635:Histamine H2 Antagonists; D013830:Thiadiazoles