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Synthesis and evaluation of 1,2,4-triazolo[1,5-c]pyrimidine derivatives as A2A receptor-selective antagonists

✍ Scribed by Bidhan A. Shinkre; T. Santhosh Kumar; Zhan-Guo Gao; Francesca Deflorian; Kenneth A. Jacobson; William C. Trenkle

Publisher: Elsevier Science
Year: 2010
Tongue: English
Weight: 645 KB
Volume: 20
Category: Article
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2010.08.021

No coin nor oath required. For personal study only.

✦ Synopsis

Movement disorders such as Parkinson's disease and Huntington's disease are serious life-limiting and debilitating movement disorders. Their onset typically occurs from mid-life to late in life, and effective diagnostic techniques for detecting and following the disease course are lacking. Our goal is to develop receptor imaging agents for positron emission tomography (PET) that selectively target the most relevant subtype of adenosine receptors (AR) that are highly expressed in the striatum, that is, the A 2A AR. To further this goal, we have synthesized and characterized pharmacologically a family of high affinity A 2A AR ligands, based on the known antagonist, SCH 442416 (R = -Me), which have structural variability on the terminus (R = -Et, -i-Pr, -allyl, and others). A O-fluoroethyl analogue suitable for use as a PET tracer had a K i value of 12.4 nM and was highly selective for the A 2A AR in comparison to the A 1 and A 3 ARs.

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