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    Synthesis and structure activity relationships of chalcone based benzocycloalkanone derivatives as adenosine a 1 and/or a 2a receptor antagonists

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    Date
    2020
    Author
    Janse van Rensburg, Helena D.
    Legoabe, Lesetja J.
    Terre'Blanche, Gisella
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    Abstract
    Adenosine A1 and/or A2A receptor antagonists hold promise for the potential treatment of neurological conditions, such as Parkinson’s disease. Herein, a total of seventeen benzocycloalkanone derivatives were synthesised and evaluated for affinity towards adenosine receptors (A1 and A2A AR). The obtained results allowed for the conclusion that affinity and/or selectivity of the 2-benzylidene-1-indanone and -tetralone derivatives toward A1 and/or A2A ARs may be modulated by the nature of the substituents (either -OH, -OCH3 or morpholine) attached at position C4 of the 1-indanone core and C5 of the 1-tetralone core as well as the meta (C3’) and/or para (C4’) position(s) on ring B. Several compounds (2a–b, 3b–c and 4a–b) possessed affinity for the A1 and/or A2A AR below 10 µM. Additionally, compounds 2a, 3b and 4a were A1 AR antagonists. These results, once again, confirmed the importance of C4 methoxy-group substitution on ring A in combination with meta (C3’) and/or para (C4’) hydroxyl-group substitution ring B of the 2-benzylidene-1-indanone scaffold leading to drug-like compounds 1h and 1j with affinity in the nanomolar-range
    URI
    http://hdl.handle.net/10394/34760
    https://www.thieme-connect.com/products/ejournals/abstract/10.1055/a-1146-2996
    https://doi.org/10.1055/a-1146-2996
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    • Faculty of Health Sciences [2368]

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