433922-12-4Relevant academic research and scientific papers
Synthesis, biological assays and QSAR studies of N-(9-benzyl-2-phenyl-8-azapurin-6-yl)-amides as ligands for A1 adenosine receptors
Giorgi, Irene,Leonardi, Michele,Pietra, Daniele,Biagi, Giuliana,Borghini, Alice,Massarelli, Ilaria,Ciampi, Osele,Bianucci, Anna Maria
body text, p. 1817 - 1830 (2009/05/27)
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 hig
Synthesis, biological activity and molecular modelling of new trisubstituted 8-azaadenines with high affinity for A1 adenosine receptors
Giorgi, Irene,Bianucci, Anna Maria,Biagi, Giuliana,Livi, Oreste,Scartoni, Valerio,Leonardi, Michele,Pietra, Daniele,Coi, Alessio,Massarelli, Ilaria,Nofal, Fatena Ahmad,Fiamingo, Francesca Lidia,Anastasi, Paola,Giannini, Giuliano
, p. 1 - 9 (2007/10/03)
We describe here the synthesis and biological activity of new 8-azaadenines bearing both a phenyl group on C(2) and a 9-benzyl group substituted in the ortho position with a Cl or a F atom or a CF3 group, to verify the synergistic effect of a c
2,9-Disubstituted-N6-(arylcarbamoyl)-8-azaadenines as new selective A3 adenosine receptor antagonists: Synthesis, biochemical and molecular modelling studies
Biagi, Giuliana,Bianucci, Anna Maria,Coi, Alessio,Costa, Barbara,Fabbrini, Laura,Giorgi, Irene,Livi, Oreste,Micco, Iolanda,Pacchini, Federica,Santini, Edoardo,Leonardi, Michele,Nofal, Fatena Ahmad,Salerni, Oreste LeRoy,Scartoni, Valerio
, p. 4679 - 4693 (2007/10/03)
A number of N6-(N-arylcarbamoyl)-2-substituted-9-benzyl-8- azaadenines, obtained by a modification of the synthetic scheme used to prepare selective A1 ligands, by only three or two steps, are described. At first we prepared a series
Characterization and preliminary use of 1-, 2- and 3-methyl-5-phenyl-7-chloro-1,2,3-triazolo[4,5-d]pyrimidine as reaction intermediates
Biagi, Giuliana,Giorgi, Irene,Livi, Oreste,Scartoni, Valerio,Barili, Pier Luigi
, p. 551 - 556 (2007/10/03)
This paper reports synthesis and characterization, by spectroscopic methods, of three new N-methyl-5-phenyl-7-chloro-1,2,3-triazolo[4,5-d]pyrimidine isomers 3a, 3b and 3c. For comparison purpose the 3-benzyl-5-phenyl-7-chloro-1,2,3-triazolo[4,5-d]pyrimidi
New N6- or N(9)-hydroxyalkyl substituted 8-azaadenines or adenines as effective A1 adenosine receptor ligands.
Biagi, Giuliana,Giorgi, Irene,Leonardi, Michele,Livi, Oreste,Pacchini, Federica,Scartoni, Valerio,Costa, Barbara,Lucacchini, Antonio
, p. 801 - 810 (2007/10/03)
In this paper we describe synthesis and biological assays of some A(1) ligands more water-soluble than the effective, but very lipophilic, 8-azaadenines and adenines discovered in the past and obtained introducing on N(6) or N(9) substituent a hydroxy group. Five of the new N(6)-hydroxyalkyl- and N(6)-hydroxycycloalkyl-2-phenyl-9-benzyl-8-azaadenines showed very high affinity (Ki40 nM) and selectivity for A(1) adenosine receptors. Among the 2-phenyl-9-(2-hydroxy-3-alkyl)-8-azaadenines or adenines prepared, the compounds with the higher A(1) affinity and selectivity resulted 2-phenyl-9-(2-hydroxy-3-propyl)-N(6)-cyclopentyl- and cyclohexyl-8-azaadenine with Ki 2.2+/-0.2 nM and 2.8+/-0.3 nM respectively. From the point of view of water-solubility, 2-phenyl-9-(2-hydroxy-3-propyl)-8-azaadenine was the most interesting compound, having a CLogP of 1.066991 and a water-solubility of 1.2 mg mL(-1).
N6-cycloalkyl-2-phenyl-3-deaza-8-azaadenines: a new class of A1 adenosine receptor ligands. A comparison with the corresponding adenines and 8-azaadenines.
Biagi, Giuliana,Giorgi, Irene,Livi, Oreste,Nardi, Antonio,Pacchini, Federica,Scartoni, Valerio,Lucacchini, Antonio
, p. 983 - 990 (2007/10/03)
Several 9-benzyl-N6-cycloalkyl-2-phenyladenines, 9-benzyl-N6-cycloalkyl-2-phenyl-8-azaadenines and 4-cycloalkylamino-1-benzyl-6-phenyl-1H-1,2,3-triazolo[4,5-c]pyridines were prepared and assayed as A1 adenosine receptor ligands. The 1H-1,2,3-triazolo[4,5-
