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

• Tipo: Artigo em Revista Científica Internacional
• Data: 2009

Autores

Maria C Carmen Balo (Autor) Outra; Jose Brea (Autor) Outra; Olga Caamano (Autor) Outra; Franco Fernandez (Autor) Outra; Xerardo Garcia Mera (Autor) Outra; Carmen Lopez (Autor) Outra; Maria I Isabel Loza (Autor) Outra; Maria I Isabel Nieto (Autor) Outra; Jose Enrique Rodriguez Borges (Autor) FCUP

Revista

Título: Bioorganic and Medicinal Chemistry

Vol. 17

Páginas: 6755-6760

ISSN: 0968-0896

Editora: Elsevier

Indexação

ISI Web of Knowledge - 10 Citações

Scopus - 13 Citações

Classificação Científica

FOS: Ciências exactas e naturais > Química

Outras Informações

ID Authenticus: P-003-FRT

DOI: 10.1016/j.bmc.2009.07.034

Abstract (EN): The synthesis of an important set of 3-furfurylxanthine derivatives is described. Binding affinities were determined for rat A(1) and human A(2A), A(2B) and A(3) receptors. Several of the 3-furfuryl-7-methylxanthine derivatives showed moderate-to-high affinity at human A(2B) receptors, the most active compound (10d) having a K(i) of 7.4 nM for hA(2B) receptors, with selectivities over rA(1) and hA(2A) receptors up to 14-fold and 11-fold, respectively. Affinities for hA(3) receptors were very low for all members of the set.

Idioma: Inglês

Tipo (Avaliação Docente): Científica

Nº de páginas: 6