- Synthesis of [1,2,4]triazolo[1,5-a]pyrazines as adenosine A2A receptor antagonists
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Potent and selective antagonists of the adenosine A2A receptor often contain a nitrogen-rich fused-ring heterocyclic core. Replacement of the core with an isomeric ring system has previously been shown to improve target affinity, selectivity, and in vivo activity. This paper describes the preparation, by a novel route, of A2A receptor antagonists containing the [1,2,4]triazolo[1,5-a]pyrazine nucleus, which is isomeric with the [1,2,4]triazolo[1,5-c]pyrimidine core of a series of known A2A antagonists with in vivo activity in animal models of Parkinson's disease.
- Dowling, James E.,Vessels, Jeffrey T.,Haque, Serajul,He, Xi Chang,Van Vloten, Kurt,Kumaravel, Gnanasambandam,Engber, Thomas,Jin, Xiaowei,Phadke, Deepali,Wang, Joy,Ayyub, Eman,Petter, Russell C.
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p. 4809 - 4813
(2007/10/03)
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- TRIAZOLOPYRAZINES AND METHODS OF MAKING AND USING THE SAME
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The invention is based on the discovery that compounds of formula (I) possess unexpectedly high affinity for the A2a adenosine receptor, and can be useful as antagonists thereof for preventing and/or treating numerous diseases, including Parkinson's disease. In one embodiment, the invention features a compound of formula I (See formula on paper copy)
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