Synthesis and pharmacological evaluation of novel substituted 9-deazaxanthines as A(2B) receptor antagonists

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

Authors

Isabel Nieto, MI (Author) Other; Carmen Balo, MC (Author) Other; Brea, J (Author) Other; Caamano, O (Author) Other; Fernandez, F (Author) Other; Garcia Mera, X (Author) Other; Lopez, C (Author) Other; Isabel Loza, MI (Author) Other; Rodriguez Borges, JE (Author) FCUP; Vidal, B (Author) Other

Journal

Title: European Journal of Medicinal Chemistry

Vol. 45 No. 7

Pages: 2884-2892

ISSN: 0223-5234

Publisher: Elsevier

Indexing

ISI Web of Knowledge - 5 Citations

Scopus - 8 Citations

Scientific classification

FOS: Engineering and technology > Chemical engineering

CORDIS: Physical sciences > Chemistry > Analytical chemistry > Clinical chemistry ; Physical sciences > Chemistry > Organic chemistry ; Health sciences > Neuroscience > Neurochemistry

Other information

Authenticus ID: P-003-56Y

DOI: 10.1016/j.ejmech.2010.03.011

Abstract (EN): 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).

Language: English

Type (Professor's evaluation): Scientific

No. of pages: 9