Evaluation of 2 ‐benzylidene‐1‐tetralone derivatives as antagonists of A1 and A2A adenosine receptors

In conclusion, the 2‐benzylidene‐1‐tetralone derivatives can be considered as lead compounds to design a new class of dual acting adenosine A1/A2A receptor antagonists that may have potential in treating both dementia and locomotor deficits in Parkinson's disease. This article is protected by copyright. All rights reserved. Substitution of 2‐benzylidene‐1‐tetralone with a hydroxy group on ring A and/or B played a key role in modulating the binding affinity and selectivity for the adenosine A1 and A2A receptors. Generally, C5‐hydroxy substitution on ring A favored A1 affinity, while C4′‐hydroxy substitution on ring B governed both A1 and A2A affinity. Adenosine A1 and A2A receptor antagonists are deemed therapeutically beneficial in Parkinson's disease; thus, 2‐benzylidene‐1‐tetralones represent a new class of dual acting adenosine A1 and A2A receptor antagonists.
Source: Chemical Biology and Drug Design - Category: Biology Authors: Tags: Research Article Source Type: research