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

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

Journal

Title: Bioorganic and Medicinal Chemistry

Vol. 18

Pages: 2001-2009

ISSN: 0968-0896

Publisher: Elsevier

Indexing

ISI Web of Knowledge - 6 Citations

Scopus - 6 Citations

Scientific classification

FOS: Natural sciences > Chemical sciences

Other information

Authenticus ID: P-003-8EZ

DOI: 10.1016/j.bmc.2010.01.028

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 A(1), A(2A), A(2)B and A(3) subtypes. Several of the 1,3,8- and 1,3,7,8-substituted xanthines showed moderate-to-high affinity at human A(2B) and A(1) receptors, with the most active compound (14q) having a pK(i) of 7.57 nM for hA(2B) receptors and a selectivity over hA(2A) receptors of 8.1-fold and hA(1) receptors of 3.7-fold.

Language: English

Type (Professor's evaluation): Scientific

No. of pages: 9