Synthesis of [1, 2, 4] triazolo [1, 5-a] pyrazines as adenosine A 2A receptor antagonists

…, T Engber, X Jin, D Phadke, J Wang, E Ayyub…

Index: 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. Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 21 p. 4809 - 4813

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Citation Number: 24

Abstract

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] ...

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