153901-93-0Relevant articles and documents
Isocytosine H2-receptor histamine antagonists. IV. The synthesis and biological activity of donetidine (SK and F 93574) and related compounds
Brown, T. H.,Blakemore, R. C.,Durant, G. J.,Ganellin, C. R.,Parsons, M. E.,et al.
, p. 601 - 608 (1993)
The synthesis and biological activity of some novel 2-amino-4-pyrimidone derivatives is described.Side-chains associated with H2 antagonist activity are attached through the 2-amino group, whilst a range of 2-hydroxypyridine containing moieties are substituted at the 5-position of the pyrimidone ring.Good H2-receptor histamine antagonist activity is observed with all the series and the majority of the compounds are selective for the H2-receptor.High aqueous solubility and iv potency coupled with an extended duration of biological activity in animal models ledto compound 16c, 2--5-(2-hydroxypyrid-4-ylmethyl)-4-pyrimidone (donetidine, SK and F 93574) being selected for clinical investigation as a potential parenterally administered therapeutic agent.H2-receptor antagonists / 2-amino-4-pyrimidones (isocytosines / imidazoles / thiazoles / pyridines / furans / 2-guanidinothiazoles / donetidine (SK and F 93574)