Synthesis of theophylline derivatives and study of their activity as antagonists at adenosine receptors

• Tipo: Artigo em Revista Científica Internacional
• Data: 2010

Autores

J. Hierrezuelo (Autor) Outra; J.M. López-Romero (Autor) Outra; R. Rico (Autor) Outra; J. Brea (Autor) Outra; M.I. Loza (Autor) Outra; C. Cai (Autor) Outra; M. Algarra (Autor) FCUP

Revista

Título: Bioorganic and Medicinal Chemistry

Vol. 18 Nº 6

Páginas: 2081-2088

ISSN: 0968-0896

Editora: Elsevier

Indexação

ISI Web of Science

Classificação Científica

FOS: Ciências da engenharia e tecnologias > Outras ciências da engenharia e tecnologias

Outras Informações

Abstract (EN): The synthesis of oligo(ethylene glycol)-alkene substituted theophyllines in positions 7 and/or 8 is described. The binding activity at adenosine receptors of selected derivatives was studied. Compound 2 showed high affinity for human A(2B) receptor (K-i = 4.16 nM) with a selectivity Ki(A2A)/Ki(A2B) of 24.1, and a solubility in water of 1 mM. The alkenyl substituent in some of the theophylline derivatives allows for covalent attachment of them onto hydrogen-terminated silicon substrate surfaces via hydrosilylation. Alternatively, an azido group was incorporated to an oligo(ethylene glycol) theophylline derivative as an anchor for tethering the molecules on ethynyl presenting surfaces via click reaction.

Idioma: Inglês

Tipo (Avaliação Docente): Científica