Synthesis of novel 1-alkyl-8-substituted-3-(3-methoxypropyl) xanthines as putative A2B receptor antagonists |
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| Authors: | María Isabel Nieto María Carmen Balo José Brea Olga Caamaño María Isabel Cadavid Franco Fernández Xerardo García Mera Carmen López José Enrique Rodríguez-Borges |
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| Institution: | 1. Departamento de Química Fundamental, Facultade de Química, Universidade de A Coruña, Campus da Zapateira, 15071 A Coruña, Spain;2. Departamento de Química Orgánica, Facultade de Farmacia, Universidade de Santiago de Compostela, E-15782 Santiago de Compostela, Spain;3. Departamento de Farmacología, Facultade de Farmacia, Universidade de Santiago de Compostela, E-15782 Santiago de Compostela, Spain;4. Instituto de Farmacia Industrial, Facultade de Farmacia, Universidade de Santiago de Compostela, E-15782 Santiago de Compostela, Spain;5. CIQ-Departamento de Química, Facultade de Ciencias, Universidade de Porto, Rua do Campo Alegre, 687, 4169-007 Porto, Portugal |
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| Abstract: | In order to identify a high-affinity, selective antagonist for the A2B subtype adenosine receptor, more than 40 1,8-disubstituted-3-(3-methoxypropyl) xanthines were prepared and evaluated for their binding affinity at recombinant human adenosine receptors, mainly of the A2A and A2B subtypes. Some of the 1-ethyl-3-(3-methoxypropyl)-8-aryl substituted derivatives 15(a–m) showed moderate-to-high affinity at human A2B receptors, with compound 15d showing A2B selectivity over the other A receptors assayed (A1, A2A, A3) of 34-fold or over. |
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