Carbamate substituted 2-amino-4,6-diphenylpyrimidines as adenosine receptor antagonists.
Basic Information
ID: ALA3751667
Journal: Bioorg Med Chem Lett
Title: Carbamate substituted 2-amino-4,6-diphenylpyrimidines as adenosine receptor antagonists.
Authors: Robinson SJ, Petzer JP, Rousseau AL, Terre'Blanche G, Petzer A, Lourens AC.
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.
CiteXplore: 26776359
DOI: 10.1016/j.bmcl.2016.01.004
Patent ID: ┄