138128-84-4

Upstream product

• 394-47-8 2-fluorobenzonitrile 

Downstream Products

• 1589081-25-3 4-amino-6-(benzo[d][1,3]dioxol-5-yl)-2-((2-(2-fluorophenyl)thiazol-4-yl)methylthio)pyrimidine-5-carbonitrile 
• 1589081-26-4 4-amino-6-(benzo[d][1,3]dioxol-5-yl)-2-((2-(4-trifluoromethylphenyl)-thiazol-4-yl)methylthio)pyrimidine-5-carbonitrile 
• 131337-33-2 {3-[2-(2-Fluoro-phenyl)-thiazol-4-ylmethyl]-4-oxo-3,4-dihydro-phthalazin-1-yl}-acetic acid 

Relevant academic research and scientific papers

Agonists for the adenosine A1 receptor with tunable residence time. a case for nonribose 4-amino-6-aryl-5-cyano-2-thiopyrimidines

We report the synthesis and evaluation of previously unreported 4-amino-6-aryl-5-cyano-2-thiopyrimidines as selective human adenosine A 1 receptor (hA1AR) agonists with tunable binding kinetics, this without affecting their nanomolar affinity for the target receptor. They show a very diverse range of kinetic profiles (from 1 min (compound 52) to 1 h (compound 43)), and their structure-affinity relationships (SAR) and structure-kinetics relationships (SKR) were established. When put in perspective with the increasing importance of binding kinetics in drug discovery, these results bring new evidence of the consequences of affinity-only driven selection of drug candidates, that is, the potential elimination of slightly less active compounds that may display preferable binding kinetics.