Synthesis and pharmacological evaluation of novel 1,3,8- and 1,3,7,8-substituted xanthines as adenosine receptor antagonists

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 hu...

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Detalhes bibliográficos
Autor principal: José Enrique Rodríguez-Borges (author)
Outros Autores: Xerardo García-Mera (author), María Carmen Balo (author), José Brea (author), Olga Caamaño (author), Franco Fernández (author), Carmen López (author), María Isabel Loza (author), María Isabel Nieto (author)
Formato: article
Idioma:eng
Publicado em: 2010
Assuntos:
Química orgânica, Química clínica, Engenharia química
Organic chemistry, Clinical chemistry, Chemical engineering
Texto completo:https://hdl.handle.net/10216/95283
País:Portugal
Oai:oai:repositorio-aberto.up.pt:10216/95283
Descrição
Resumo: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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