Synthesis and pharmacological evaluation of novel substituted 9-deazaxanthines as A2B receptor antagonists

María Isabel Nieto; María Carmen Balo; José Brea; Olga Caamaño; Franco Fernández; Xerardo García-Mera; Carmen López; María Isabel Loza; José Enrique Rodríguez-Borges; Bernat Vidal

doi:10.1016/j.ejmech.2010.03.011

Synthesis and pharmacological evaluation of novel substituted 9-deazaxanthines as A2B receptor antagonists

Eur J Med Chem. 2010 Jul;45(7):2884-92. doi: 10.1016/j.ejmech.2010.03.011. Epub 2010 Mar 12.

Authors

María Isabel Nieto¹, María Carmen Balo, José Brea, Olga Caamaño, Franco Fernández, Xerardo García-Mera, Carmen López, María Isabel Loza, José Enrique Rodríguez-Borges, Bernat Vidal

Affiliation

¹ Departamento de Química Fundamental, Facultade de Química, Universidade de A Coruña, Campus da Zapateira, E-15071, A Coruña, Spain.

PMID: 20371139
DOI: 10.1016/j.ejmech.2010.03.011

Abstract

A new series of 9-deazaxanthine derivatives with various substituents at the heterocyclic system were synthesized and evaluated for their binding affinities for the four human recombinant adenosine receptors, A(1)-A(3) subtypes. A number of the 9-deazaxanthines derivatives 3a-m showed moderate-to-high affinity for hA(2B) receptors, with compound 3f showing a 32-fold selectivity for A(2B) over A(1) and a 2750-fold selectivity for A(2B) over A(2A).

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Adenosine A2 Receptor Antagonists*
Animals
CHO Cells
Cricetinae
Cricetulus
HeLa Cells
Humans
Ligands
Xanthines / chemical synthesis*
Xanthines / chemistry
Xanthines / pharmacology*

Substances

Adenosine A2 Receptor Antagonists
Ligands
Xanthines