Robinson, Sarel J.Petzer, Jacobus P.Terre'Blanche, GisellaPetzer, AnélLourens, Anna C.U.Rousseau, Amanda L.2017-05-152017-05-152016Robinson, S.J. et al. 2016. Carbamate substituted 2-amino-4,6-diphenylpyrimidines as adenosine receptor antagonists. Bioorganic & medicinal chemistry letters, 26:734-738. [https://doi.org/10.1016/j.bmcl.2016.01.004]0960-894X1464-3405 (Online)http://hdl.handle.net/10394/23160https://www.sciencedirect.com/science/article/pii/S0960894X1630004Xhttps://doi.org/10.1016/j.bmcl.2016.01.004A 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 optimisation2-AminopyrimidineAdenosine A1 and A2A receptorDualAntagonistArticle