Structure–activity relationships in a series of 8-substituted xanthines as A 1-adenosine receptor antagonists

…, S Corsano, R Barbaro, G Giannaccini, L Betti

Index: Strappaghetti, Giovannella; Corsano, Stefano; Barbaro, Roberta; Giannaccini, Gino; Betti, Laura Bioorganic and Medicinal Chemistry, 2001 , vol. 9, # 3 p. 575 - 583

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Citation Number: 17

Abstract

A series of 8-substituted xanthines were synthesized and their affinity in vitro towards A1, A2A-adenosine receptors was evaluated by radioligand receptor binding assays. All compounds showed a greater affinity and selectivity towards the A1-adenosine receptor than theophylline. The compounds in which the n-proyl group is in 1-position of the xanthine nucleus and the pyridazinone system in 8-position is linked through a chain of two or four ...