Impact of the aryl substituent kind and distance from pyrimido[2,1-f]purindiones on the adenosine receptor selectivity and antagonistic properties.
Adenosine receptor (AR) antagonists belong to two major groups of compounds: xanthines and non-xanthines. Recently several annelated xanthine derivatives have been described as selective A(1), A(2A), A(2B) and A(3) ARs antagonists. Contrary to dipropyl derivatives, in the group of dimethyl (un)substituted arylalkyl pyrimido[2,1-f]purindiones selective mainly adenosine A(2A) receptor antagonists were identified. Their activity depended on aryl substitution and its distance from pyrimido[2,1-f]purindione.
Faculty of Pharmacy, Department of Chemical Technology of Drugs, Jagiellonian University Medical College, Medyczna 9, PL 30-688, Krakow, Poland.
Anna
A
Drabczyńska
Britta
B
Schumacher
Christa E
CE
Müller
Janina
J
Karolak-Wojciechowska
Barbara
B
Michalak
Elzbieta
E
Pekala
Katarzyna
K
Kieć-Kononowicz
D058917:Adenosine A2 Receptor Antagonists; D000818:Animals; D006801:Humans; D015394:Molecular Structure; D058915:Purinergic P1 Receptor Antagonists; D011687:Purines / Q000737:chemistry* / Q000378:metabolism* / Q000494:pharmacology; D011743:Pyrimidines / Q000737:chemistry* / Q000378:metabolism* / Q000494:pharmacology; D051381:Rats; D043705:Receptor, Adenosine A2A / Q000378:metabolism; D018047:Receptors, Purinergic P1 / Q000378:metabolism; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D013806:Theophylline / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D014970:Xanthines / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology
D058917:Adenosine A2 Receptor Antagonists; D058915:Purinergic P1 Receptor Antagonists; D011687:Purines; D011743:Pyrimidines; D043705:Receptor, Adenosine A2A; D018047:Receptors, Purinergic P1; D014970:Xanthines; D013806:Theophylline