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

• Type: Article in International Scientific Journal
• Date: 2009

Authors

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

Journal

Title: Bioorganic and Medicinal Chemistry

Vol. 17

Pages: 6755-6760

ISSN: 0968-0896

Publisher: Elsevier

Indexing

ISI Web of Knowledge - 10 Citations

Scopus - 13 Citations

Scientific classification

FOS: Natural sciences > Chemical sciences

Other information

Authenticus ID: 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.

Language: English

Type (Professor's evaluation): Scientific

No. of pages: 6