Pyrazolo[1',5':1,6]pyrimido[4,5-d]pyridazin-4(3H)-ones as selective human A(1) adenosine receptor ligands |
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Authors: | Giovannoni Maria Paola Vergelli Claudia Cilibrizzi Agostino Crocetti Letizia Biancalani Claudio Graziano Alessia Dal Piaz Vittorio Loza Maria Isabel Cadavid Maria Isabel Díaz José Luis Gavaldà Amadeu |
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Affiliation: | Dipartimento di Scienze Farmaceutiche, via Ugo Schiff 6, 50019 Sesto Fiorentino Firenze, Italy. mariapaola.giovannoni@unifi.it |
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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. |
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