Synthesis and pharmacological evaluation of novel 1,3,8- and 1,3,7,8-substituted xanthines as adenosine receptor antagonists |
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| Authors: | José Enrique Rodríguez-Borges Xerardo García-Mera María Carmen Balo José Brea Olga Caamaño Franco Fernández Carmen López María Isabel Loza María Isabel Nieto |
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| Affiliation: | 1. CIQ-Departamento de Química, Facultade de Ciencias, Universidade de Porto, Rua do Campo Alegre, 687, 4169-007 Porto, Portugal;2. Departamento de Química Orgánica, Facultade de Farmacia, Universidade de Santiago de Compostela, E-15782 Santiago de Compostela, Spain;3. Instituto de Farmacia Industrial, Facultade de Farmacia, Universidade de Santiago de Compostela, E-15782 Santiago de Compostela, Spain;4. Departamento de Farmacología, Facultade de Farmacia, Universidade de Santiago de Compostela, E-15782 Santiago de Compostela, Spain;5. Departamento de Química Fundamental, Facultade de Química, Universidade de A Coruña, Campus da Zapateira, 15071, A Coruña, Spain |
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| Abstract: | A number of novel xanthines bearing a variety of substituents at positions 1, 3, 7 and 8 were prepared and evaluated for their binding affinity to the human adenosine receptor A1, A2A, A2B and A3 subtypes. Several of the 1,3,8- and 1,3,7,8-substituted xanthines showed moderate-to-high affinity at human A2B and A1 receptors, with the most active compound (14q) having a pKi of 7.57 nM for hA2B receptors and a selectivity over hA2A receptors of 8.1-fold and hA1 receptors of 3.7-fold. |
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