A New Series of 2-Alkoxy(aralkoxy)-[1,2,4]triazolo[1,5-a]quinazolin-5-ones as Adenosine Receptor Antagonists

作者：Al Salahi Rashad^*; Geffken Detlef; Koellner Maria

来源：Chemical & Pharmaceutical Bulletin, 2011, 59(6): 730-733.

DOI：10.1248/cpb.59.730

• 1,2,4-triazoloquinazoline
• adenosine receptor
• radioligand binding affinity

This research was carried out to study the pharmacological activity of a newly synthesized series of 2-alkoxy-[1,2,4]triazolo[1,5-a]quinazolin-5-ones as adenosine receptor antagonists. These compounds have been tested in radioligand binding assays on cloned Chinese hamster ovary (CHO) cells transfected with A(1), A(2A), A(2B) and A(3) receptors. In particular, among the triazoloquinazolines (1-11), the dialkoxy derivative (7b) was found to have the highest affinity at A(1) subtype receptor, and its radioligand binding activity together with 1,3-dipropyl-8-cyclopentylxanthine (DPCPX) was studied. Finally, the structure activity relationship (SAR) studies on the titled compounds provide some new insights about steric hindrance and lipophilic requirements for anchoring to the adenosine receptors recognition site.

• 出版日期2011-6