Synthesis and pharmacological evaluation of novel 1- and 8-substituted-3-furfuryl xanthines as adenosine receptor antagonists |
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| Authors: | Marí a Carmen Balo, Jos Brea, Olga Caama o, Franco Fern ndez, Xerardo Garcí a-Mera, Carmen L pez, Marí a Isabel Loza, Marí a Isabel Nieto,Jos Enrique Rodrí guez-Borges |
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| Affiliation: | María Carmen Balo, José Brea, Olga Caamaño, Franco Fernández, Xerardo García-Mera, Carmen López, María Isabel Loza, María Isabel Nieto,José Enrique Rodríguez-Borges |
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| Abstract: | The synthesis of an important set of 3-furfurylxanthine derivatives is described. Binding affinities were determined for rat A1 and human A2A, A2B and A3 receptors. Several of the 3-furfuryl-7-methylxanthine derivatives showed moderate-to-high affinity at human A2B receptors, the most active compound (10d) having a Ki of 7.4 nM for hA2B receptors, with selectivities over rA1 and hA2A receptors up to 14-fold and 11-fold, respectively. Affinities for hA3 receptors were very low for all members of the set. |
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| Keywords: | 3-Furfuryl xanthines Synthesis Adenosine receptor antagonist A2B, A2A and A3 Binding affinities |
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