Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1370047 | Bioorganic & Medicinal Chemistry Letters | 2016 | 5 Pages |
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.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Sarel J. Robinson, Jacobus P. Petzer, Amanda L. Rousseau, Gisella Terre’Blanche, Anél Petzer, Anna C.U. Lourens,