Abstract:
:2-Phenyl-9-benzyl-8-azapurines, bearing at the 6 position an amido group interposed between the 8-azapurine moiety and an alkyl or a substituted phenyl group, have been synthesised and assayed as ligands for adenosine receptors. All the compounds show high affinity for the A(1) adenosine receptor, and many of them also show a good selectivity for A(1) with respect to A(2A) and A(3) adenosine receptors. Based on the quite rich library containing such compounds and relevant biological data, QSAR models, able to rationalise the results and to give a quantitative estimate of the observed trends were also developed. The obtained models can assist in the design of new compounds selectively active on A(1) adenosine receptor.
journal_name
Bioorg Med Chemjournal_title
Bioorganic & medicinal chemistryauthors
Giorgi I,Leonardi M,Pietra D,Biagi G,Borghini A,Massarelli I,Ciampi O,Bianucci AMdoi
10.1016/j.bmc.2009.01.060subject
Has Abstractpub_date
2009-03-01 00:00:00pages
1817-30issue
5eissn
0968-0896issn
1464-3391pii
S0968-0896(09)00105-9journal_volume
17pub_type
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