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Eur J Med Chem. 2013 May;63:924-34. doi: 10.1016/j.ejmech.2013.03.020. Epub 2013 Mar 22.

New insight into adenosine receptors selectivity derived from a novel series of [5-substituted-4-phenyl-1,3-thiazol-2-yl] benzamides and furamides.

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1
Department of Medicinal Chemistry, B.V. Patel Pharmaceutical Education and Research Development, Ahmedabad 380 054, Gujarat, India.

Abstract

A series of [5-substituted-4-phenyl-1,3-thiazol-2-yl] benzamide and furamide analogues were investigated in radioligand binding studies at adenosine receptor subtypes with an aim to obtain potent and selective adenosine receptor ligands. Benzamide and furamide linked to thiazole was found to be crucial for high adenosine receptor affinity. The most potent compound indentified in this study was 5d with low nanomolar affinity for all four adenosine receptor subtypes. Compounds 5a and 5g showed moderate selectivity for A2A adenosine receptors. Molecular docking versus all four human adenosine receptors combined with membrane molecular dynamics studies were performed to rationalise the peculiar selectivity profile of 5d antagonist.

PMID:
23685887
DOI:
10.1016/j.ejmech.2013.03.020
[Indexed for MEDLINE]
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