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    Carbamate substituted 2-amino-4,6-diphenylpyrimidines as adenosine receptor antagonists

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    Date
    2016
    Author
    Robinson, Sarel J.
    Petzer, Jacobus P.
    Terre'Blanche, Gisella
    Petzer, Anél
    Lourens, Anna C.U.
    Rousseau, Amanda L.
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    Abstract
    A novel series of carbamate substituted 2-amino-4,6-diphenylpyrimidines was evaluated as potential dual adenosine A1 and A2A receptor antagonists. The majority of the synthesised compounds exhibited promising dual affinities, with A1Ki values ranging from 0.175 to 10.7 nM and A2AKi values ranging from 1.58 to 451 nM. The in vivo activity illustrated for 3-(2-amino-6-phenylpyrimidin-4-yl)phenyl morpholine-4-carboxylate (4c) is indicative of the potential of these compounds as therapeutic agents in the treatment of Parkinson’s disease, although physicochemical properties may require optimisation
    URI
    http://hdl.handle.net/10394/23160
    https://www.sciencedirect.com/science/article/pii/S0960894X1630004X
    https://doi.org/10.1016/j.bmcl.2016.01.004
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