Synthesis of 4,6-disubstituted- and 4,5,6-trisubstituted-2-phenyl-pyrimidines and their affinity towards A1 adenosine receptors.
Synthesis and assay of title compounds are reported. The results can support our hypothesis about the possibility that molecules characterized by great flexibility, as the title 2-phenyl-4,5,6-triaminopyrimidines, can better interact with the receptor sites compared with rigid molecules as 2,6,9-trisubstituted 8-azaadenines. Relatively low activity shown by pyrimidine derivatives demonstrated the importance of the bicyclic aromatic system in 8-azaadenines and adenines to give a favourable interaction between a hexogenous molecule and the A1 adenosine receptors.
Biagi
G
G
Dipartimento di Scienze Farmaceutiche, Università di Pisa, Italy.
Giorgi
I
I
Livi
O
O
Scartoni
V
V
Lucacchini
A
A
D000818:Animals; D001921:Brain / Q000187:drug effects / Q000378:metabolism; D002417:Cattle; D066298:In Vitro Techniques; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000494:pharmacology; D011869:Radioligand Assay; D018047:Receptors, Purinergic P1 / Q000378:metabolism*; D013055:Spectrophotometry, Infrared
D011743:Pyrimidines; D018047:Receptors, Purinergic P1