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

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-4 H -chromene-2-carboxamide to...

Full description

Saved in:
Bibliographic Details
Published in:RSC advances 2016, Vol.6 (52), p.46972-46976
Main Authors: Cagide, F., Reis, J., Gaspar, A., Chavarria, D., Kachler, S., Klotz, K. N., Gomes, L. R., Low, J. N., Vilar, S., Hripcsak, G., Borges, F.
Format: Article
Language:English
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary: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-4 H -chromene-2-carboxamide to the hA 1 AR ( K i = 0.219 μM) and reinforce the crucial role of AR affinity of the amide linker located at C-2 of the pyrone ring.
ISSN:2046-2069
2046-2069
DOI:10.1039/C6RA02347A