640274-34-6Relevant academic research and scientific papers
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-
Synthesis and structure-activity relationships of 2-substituted-8-hydroxyadenine derivatives as orally available interferon inducers without emetic side effects
Isobe, Yoshiaki,Tobe, Masanori,Ogita, Haruhisa,Kurimoto, Ayumu,Ogino, Tetsuhiro,Kawakami, Hajime,Takaku, Haruo,Sajiki, Hironao,Hirota, Kosaku,Hayashi, Hideya
, p. 3641 - 3647 (2007/10/03)
Recently we reported the adenine derivatives (2-4) as new interferon (IFN) inducers. In the present study, we conducted a detailed structure and activity relationship study of 4 and its related derivatives on IFN inducing activity. From this study, we found that compound 4 exhibited the most potent IFN inducing activity in vitro with a minimum effective concentration of 0.01 μM, and 4 also showed strong IFN-inducing activity at doses of more than 0.3 mg/kg by oral administration in mice. This potency was 10-fold stronger than that of Imiquimod. Moreover, 4 did not cause emesis in ferrets even at doses as high as 10 mg/kg, whereas, 80% of animals were emetic when orally administered with the same dose of Imiquimod. These results indicate that compound 4 is superior to Imiquimod with respect to efficacy and safety.
