651310-88-2

Upstream product

• 1603-41-4 (5-methyl-pyridin-2-yl)amine 
• 58092-40-3 2-benzenesulfonyl-3,3-bis(methylsulfanyl)acrylonitrile 
• 76-05-1 trifluoroacetic acid 

Relevant academic research and scientific papers

Structure activity relationship studies of 3-arylsulfonyl-pyrido[1,2-a] pyrimidin-4-imines as potent 5-HT6 antagonists

Comprehensive structure activity relationship (SAR) studies were conducted on a focused screening hit, 2-(methylthio)-3-(phenylsulfonyl)-4H-pyrido[1,2-a] pyrimidin-4-imine (1, IC50: 4.0 nM), as 5-HT6 selective antagonists. Activity was improved some 2-4 fold when small, electron-donating groups were added to the central core as observed in 19, 20 and 26. Molecular docking of key compounds in a homology model of the human 5-HT6 receptor was used to rationalize our structure-activity relationship (SAR) findings. In pharmacokinetic experiments, compound 1 displayed good brain uptake in rats following intra-peritoneal administration, but limited oral bioavailability.

Pyridopyrimidine derivatives as 5-HT6 antagonists

Novel pyridopyrimidine derivatives which have a binding affinity for the human 5-HT6 receptor and, therefore, are useful in treating disorders responsive to antagonism of the 5-HT6 receptor such as psychosis, schizophrenia, manic depression, depression, neurological disorder, memory disorder, Parkinson's disease, amyotrophic lateral sclerosis, Alzheimer's disease and Huntington's chorea.