title: 1,2,3-triazole[4,5-d]pyridazines--IV. Preparation and adenosine receptor binding of new 4 and/or 7 aminoderivatives.
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(+)-alpha-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.
authors.affiliation: Istituto di Chimica Farmaceutica e Tossicologica, Università di Pisa.
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: S
authors.initials: S
authors.lastname: Velo
authors.forename: C
authors.initials: C
authors.lastname: Martini
authors.forename: G
authors.initials: G
authors.lastname: Senatore
authors.forename: P L
authors.initials: PL
authors.lastname: Barili
mesh_terms: D000818:Animals; D001921:Brain / Q000378:metabolism; D011724:Pyridazines / Q000737:chemistry* / Q000378:metabolism; D051381:Rats; D018047:Receptors, Purinergic P1 / Q000378:metabolism*; D012756:Sheep; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000737:chemistry* / Q000378:metabolism
chemical_list: D011724:Pyridazines; D018047:Receptors, Purinergic P1; D014230:Triazoles