title: Synthesis of 4,6-disubstituted- and 4,5,6-trisubstituted-2-phenyl-pyrimidines and their affinity towards A1 adenosine receptors.
abstract: 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.
authors.affiliation: Dipartimento di Scienze Farmaceutiche, Università di Pisa, Italy.
authors.forename: G
authors.initials: G
authors.lastname: Biagi
authors.forename: I
authors.initials: I
authors.lastname: Giorgi
authors.forename: O
authors.initials: O
authors.lastname: Livi
authors.forename: V
authors.initials: V
authors.lastname: Scartoni
authors.forename: A
authors.initials: A
authors.lastname: Lucacchini
mesh_terms: 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
chemical_list: D011743:Pyrimidines; D018047:Receptors, Purinergic P1