129528-46-7Relevant academic research and scientific papers
Isocytosine H2-receptor histamine antagonists. III. The synthesis and biological activity of lupitidine (SK and F 93479) and related compounds
Brown,Armitage,Blakemore,Blurton,Durant,Ganellin,Ife,Parsons,Rawlings,Slingsby
, p. 217 - 226 (2007/10/02)
A series of 2-[2-(5-dimethylaminomethyl-2-furanylmethylthio)ethylamino]-4-pyrimidones is described containing a variety of substituents in the 5-position of the pyrimidone (isocytosine) ring. Good H2-receptor histamine antagonist activity is retained over a range of basic and neutral, polar and non-polar substituents and the majority of compounds are selective for the H2-receptor. Modifications have also been made to the furan ring and N,N-dimethylaminomethyl substituent and structure-activity observations are discussed. Compound (16f) 2-[2-(5-dimethylaminomethyl-2-furanylmethylthio)ethylamino]-5-(6-methyl-3- pyridylmethyl)-4-pyrimidone (SK and F 93479, lupitidine), a compound which shows an extended duration of anti-secretory activity in animal models, was selected for clinical investigation.
