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Doc ID CHEMBL1275345
Journal Bioorg Med Chem (2010) 18:7890-7899
Title Pyrazolo[1',5':1,6]pyrimido[4,5-d]pyridazin-4(3H)-ones as selective human A(1) adenosine receptor ligands.
Authors Giovannoni MP, Vergelli C, Cilibrizzi A, Crocetti L, Biancalani C, Graziano A, Dal Piaz V, Loza MI, Cadavid MI, Diaz JL, Gavalda A.
Abstract A series of pyrazolo[1',5':1,6]pyrimido[4,5-d]pyridazin-4(3H)-ones was synthesized and tested in radioligand binding assays to determine their affinities for the human adenosine A(1), A(2A), A(2B) and A(3) receptors. Results indicated that this scaffold is appropriate for adenosine receptor subtype A(1) ligands and that the best arranged groups around this scaffold are 3- and 4-pyridinyl at position 1, benzyl at position 3, hydrogen at position 6 and 3-thienyl or phenyl at position 9. The most interesting compounds showed K(i) for A1 in the nanomolar range and an appreciable selectivity for other receptor subtypes.
CiteXplore 20937560
DOI 10.1016/j.bmc.2010.09.043

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