This paper reports the continuation of the studies on the 4-aminosubstituted 1,2,3-triazole[4,5-d]pyridazine derivatives which had shown binding affinity towards adenosine receptors. Biological results confirmed the greater activity of a benzyl substituent in the 1 position and the receptorial stereoselectivity related to the higher and more selective A1 affinity of the 4-D(+)-α-methylbenzylamino enantiomer 1b. The 4-phenylhydrazino substituent has shown an interesting binding activity about equipotent towards A1 and A2 receptorial sites. A surprisingly elevated A1 affinity (Ki = 7 nM), 440 fold higher than A2 affinity, is presented by compound 1d, bearing a m-toluidino substituent.

1,2,3-Triazole[4,5-d]pyridazines IV. Preparation and Adenosine Receptor Binding of New 4-and /or 7-Aminoderivatives

GIORGI, IRENE;MARTINI, CLAUDIA;LUCACCHINI, ANTONIO
1995

Abstract

This paper reports the continuation of the studies on the 4-aminosubstituted 1,2,3-triazole[4,5-d]pyridazine derivatives which had shown binding affinity towards adenosine receptors. Biological results confirmed the greater activity of a benzyl substituent in the 1 position and the receptorial stereoselectivity related to the higher and more selective A1 affinity of the 4-D(+)-α-methylbenzylamino enantiomer 1b. The 4-phenylhydrazino substituent has shown an interesting binding activity about equipotent towards A1 and A2 receptorial sites. A surprisingly elevated A1 affinity (Ki = 7 nM), 440 fold higher than A2 affinity, is presented by compound 1d, bearing a m-toluidino substituent.
Biagi, G; Giorgi, Irene; Livi, O; Scartoni, V; Velo, S; Martini, Claudia; Senatore, G; Barili, P. L.; Lucacchini, Antonio
File in questo prodotto:
Non ci sono file associati a questo prodotto.

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11568/204250
 Attenzione

Attenzione! I dati visualizzati non sono stati sottoposti a validazione da parte dell'ateneo

Citazioni
  • ???jsp.display-item.citation.pmc??? ND
  • Scopus 14
  • ???jsp.display-item.citation.isi??? 14
social impact