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

• Type: Article in International Scientific Journal
• Date: 2010

Authors

José Enrique Rodríguez-Borges (Author) FCUP; Xerardo García-Mera (Author) Other; María Carmen Balo (Author) Other; José Brea (Author) Other; Olga Caamaño (Author) Other; Franco Fernández (Author) Other; Carmen López (Author) Other; María Isabel Loza (Author) Other; María Isabel Nieto (Author) Other

Journal

Title: Bioorganic and Medicinal Chemistry

Vol. 18 No. 5

Pages: 2001-2009

ISSN: 0968-0896

Publisher: Elsevier

Indexing

ISI Web of Knowledge - 6 Citations

Scopus - 6 Citations

Scientific classification

FOS: Engineering and technology > Chemical engineering

CORDIS: Physical sciences > Chemistry > Organic chemistry ; Physical sciences > Chemistry > Analytical chemistry > Clinical chemistry

Other information

Authenticus ID: P-003-8EZ

Abstract (EN): 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.

Language: English

Type (Professor's evaluation): Scientific