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Bioorg Med Chem Lett. 2016 Feb 15;26(4):1348-54. doi: 10.1016/j.bmcl.2015.11.048. Epub 2015 Dec 1.

Discovery of aminoquinazoline derivatives as human A(2A) adenosine receptor antagonists.

Author information

1
Department of Chemical Research, Merck Research Laboratories, 126 E. Lincoln Ave., Rahway, NJ 07065, USA.
2
Department of Chemical Research, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
3
Department of Chemical Research, Merck Research Laboratories, 770 Sumneytown Pike, West Point, PA 19486, USA.

Abstract

Novel bicyclic adenosine A(2A) antagonists with an aminoquinazoline moiety were designed and synthesized. The optimization of the initial lead compound based on in vitro and in vivo activity has led to the discovery of a potent and selective class of adenosine A(2A) antagonists. The structure-activity relationships of this novel series of bicyclic aminoquinazoline derivatives as adenosine A(2A) antagonists are described in detail.

KEYWORDS:

Adenosine A(2A) receptor antagonist; Aminoquinazoline; Parkinson’s disease

PMID:
26781932
DOI:
10.1016/j.bmcl.2015.11.048
[Indexed for MEDLINE]

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