Synthesis of novel 1-alkyl-8-substituted-3-(3-methoxypropyl) xanthines as putative A(2B) receptor antagonists

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

Authors

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

Journal

Title: Bioorganic and Medicinal Chemistry

Vol. 17

Pages: 3426-3432

ISSN: 0968-0896

Publisher: Elsevier

Indexing

ISI Web of Knowledge - 15 Citations

Scopus - 18 Citations

Scientific classification

FOS: Natural sciences > Chemical sciences

Other information

Authenticus ID: P-003-K7D

DOI: 10.1016/j.bmc.2009.03.029

Abstract (EN): In order to identify a high-affinity, selective antagonist for the A(2B) subtype adenosine receptor, more than 40 1,8-disubstituted-3-(3-methoxypropyl) xanthines were prepared and evaluated for their binding affinity at recombinant human adenosine receptors, mainly of the A(2A) and A(2B) subtypes. Some of the 1-ethyl-3-(3-methoxypropyl)-8-aryl substituted derivatives 15(a-m) showed moderate-to-high affinity at human A(2B) receptors, with compound 15d showing A(2B) selectivity over the other A receptors assayed (A(1), A(2A), A(3)) of 34-fold or over.

Language: English

Type (Professor's evaluation): Scientific

No. of pages: 7