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Bioorg Med Chem Lett. 2016 Feb 1;26(3):734-738. doi: 10.1016/j.bmcl.2016.01.004. Epub 2016 Jan 5.

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

Author information

1
Pharmaceutical Chemistry, School of Pharmacy, North-West University, Private Bag X6001, Potchefstroom 2520, South Africa; Centre of Excellence for Pharmaceutical Sciences, North-West University, Private Bag X6001, Potchefstroom 2520, South Africa.
2
Molecular Sciences Institute, School of Chemistry, University of the Witwatersrand, Private Bag 3, PO WITS 2050, South Africa.
3
Centre of Excellence for Pharmaceutical Sciences, North-West University, Private Bag X6001, Potchefstroom 2520, South Africa.
4
Pharmaceutical Chemistry, School of Pharmacy, North-West University, Private Bag X6001, Potchefstroom 2520, South Africa; Centre of Excellence for Pharmaceutical Sciences, North-West University, Private Bag X6001, Potchefstroom 2520, South Africa. Electronic address: arina.lourens@nwu.ac.za.

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.

KEYWORDS:

2-Aminopyrimidine; Adenosine A(1) and A(2A) receptor; Antagonist; Dual

PMID:
26776359
DOI:
10.1016/j.bmcl.2016.01.004
[Indexed for MEDLINE]

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