In this paper we report the synthesis and biological evaluation of a new series of pyrazolo[1',5':1,6]pyrimido[4,5-d]pyridazin-4(3H)-ones as human A1 adenosine receptor ligands. The tricyclic scaffold was modified at position 6 and 9 by introducing small alkyl chains and substituted phenyls. The most interesting compounds showed Ki for A1 in the submicromolar range (0.105-0.244 µM) and the most interesting term (compound 4c) combined an appreciable affinity for A1 (Ki = 0.132 µM) with a good selectivity toward A2A (43% inhibition at 10 µM) and A3 (46% inhibition at 10 µM).
Autori interni: | |
Autori: | Graziano A; Giovannoni MP; Cilibrizzi A; Crocetti L; Piaz VD; Vergelli C; Trincavelli ML; Martini C; Giacomelli C. |
Titolo: | New Pyrazolo[1',5':1,6]pyrimido[4,5-d]pyridazin-4(3H)-ones Fluoroderivatives as Human A1 Adenosine Receptor Ligands. |
Anno del prodotto: | 2012 |
Appare nelle tipologie: | 1.1 Articolo in rivista |
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