title: A new series of 2-alkoxy(aralkoxy)-[1,2,4]triazolo[1,5-a]quinazolin-5-ones as adenosine receptor antagonists.
abstract: 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.
authors.affiliation: Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia. salahi76@yahoo.com
authors.forename: Rashad
authors.initials: R
authors.lastname: Al-Salahi
authors.forename: Detlef
authors.initials: D
authors.lastname: Geffken
authors.forename: Maria
authors.initials: M
authors.lastname: Koellner
mesh_terms: D000818:Animals; D016466:CHO Cells; D006224:Cricetinae; D003412:Cricetulus; D058915:Purinergic P1 Receptor Antagonists / Q000737:chemistry* / Q000494:pharmacology; D052999:Quinazolinones / Q000737:chemistry* / Q000494:pharmacology; D043682:Receptor, Adenosine A1 / Q000737:chemistry / Q000378:metabolism; D043705:Receptor, Adenosine A2A / Q000737:chemistry / Q000378:metabolism; D043704:Receptor, Adenosine A2B / Q000737:chemistry / Q000378:metabolism; D043684:Receptor, Adenosine A3 / Q000737:chemistry / Q000378:metabolism; D018047:Receptors, Purinergic P1 / Q000737:chemistry* / Q000378:metabolism; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000737:chemistry*
chemical_list: D058915:Purinergic P1 Receptor Antagonists; D052999:Quinazolinones; D043682:Receptor, Adenosine A1; D043705:Receptor, Adenosine A2A; D043704:Receptor, Adenosine A2B; D043684:Receptor, Adenosine A3; D018047:Receptors, Purinergic P1; D014230:Triazoles; C045575:1,2,4-triazole