Discovery of the first A(1) adenosine receptor ligand based on the chromone scaffold

• Type: Article in International Scientific Journal
• Date: 2016

Authors

Fernando Cagide (Author) FCUP; Reis, J (Author) Other; Gaspar, A (Author) Other; Chavarria, D (Author) Other; Kachler, S (Author) Other; Klotz, KN (Author) Other; Gomes, LR (Author) Other; Low, JN (Author) Other; Vilar, S (Author) Other; Hripcsak, G (Author) Other; Fernanda Borges (Author) FCUP

Journal

Title: RSC Advances

Vol. 6

Pages: 46972-46976

ISSN: 2046-2069

Publisher: Royal Society of Chemistry

Indexing

ISI Web of Knowledge - 5 Citations

Scopus - 5 Citations

Other information

Authenticus ID: P-00K-GX6

DOI: 10.1039/c6ra02347a

Abstract (EN): The first potent and selective hA(1)AR ligand based on the chromone scaffold is reported in this work. Receptor-driven molecular modeling studies provide valuable information about the molecular interactions responsible for the high affinity of N-(2-nitrophenyl)-4-oxo-4H-chromene-2-carboxamide to the hA(1)AR (K-i = 0.219 mu M) and reinforce the crucial role of AR affinity of the amide linker located at C-2 of the pyrone ring.

Language: English

Type (Professor's evaluation): Scientific

No. of pages: 5