Evaluation of 2‐benzylidene‐1‐tetralone derivatives as antagonists of A1 and A2A adenosine receptors
作者： Lesetja J. Legoabe , Mietha M. Van der Walt , Gisella Terre'Blanche
DOI: 10.1111/CBDD.13074
关键词:
摘要: Antagonists of the adenosine receptors (A1 and A2A ) are thought to be beneficial in neurological disorders, such as Alzheimer's Parkinson's disease. The aim this study was explore 2-benzylidene-1-tetralone derivatives antagonists A1 and/or receptors. In general, test compounds were found selective for receptor, with only three possessing affinity both receptor. 2-benzylidene-1-tetralones bearing a hydroxyl substituent at either position C5, C6 or C7 ring A displayed favourable receptor binding, while C5 hydroxy substitution led affinity. Interestingly, para-hydroxy on B combination provided Compounds 4 8 highest values below 7 μm. Both these behaved performed GTP shift assays. conclusion, can considered lead design new class dual acting /A2A that may have potential treating dementia locomotor deficits
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