A series of pyrano[ 2,3-c] pyrazol-4-ones was synthesized and evaluated for bovine brain adenosine A, and A,, receptor binding affinity. Substituents at positions 5 and/or 6 were varied in order to define the structure-activity relationships in these new kinds of adenosine receptor ligands. The most selective and potent ligand among the reported compounds was the 1,4-dihydro-1-phenyl-3-methyl-6-( 3-aminophenyl)- pyrano[2,3-c] pyrazol-4-one 11 which showed a 27-fold selectivity for A(i) receptor and a K-i value of 84 nM. (C) 1998 Elsevier Science S.A. All rights reserved.
Synthesis and A(1) and A(2A) adenosine binding activity of some pyrano[2,3-c]pyrazol-4-ones
TRINCAVELLI, MARIA LETIZIA;MARTINI, CLAUDIA;LUCACCHINI, ANTONIO
1998-01-01
Abstract
A series of pyrano[ 2,3-c] pyrazol-4-ones was synthesized and evaluated for bovine brain adenosine A, and A,, receptor binding affinity. Substituents at positions 5 and/or 6 were varied in order to define the structure-activity relationships in these new kinds of adenosine receptor ligands. The most selective and potent ligand among the reported compounds was the 1,4-dihydro-1-phenyl-3-methyl-6-( 3-aminophenyl)- pyrano[2,3-c] pyrazol-4-one 11 which showed a 27-fold selectivity for A(i) receptor and a K-i value of 84 nM. (C) 1998 Elsevier Science S.A. All rights reserved.File in questo prodotto:
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