| 15341933 |
Vu CB, Pan D, Peng B, Sha L, Kumaravel G, Jin X, Phadke D, Engber T, Huang C, Reilly J, Tam S, Petter RC: Studies on adenosine A2a receptor antagonists: comparison of three core heterocycles. Bioorg Med Chem Lett. 2004 Oct 4;14(19):4831-4.
Piperazine and (R)-2-(aminomethyl) pyrrolidine derivatives of [1,2,4] triazolo [1,5-a][1,3,5] triazine have recently been shown to be potent and selective adenosine A (2a) receptor antagonists. We have replaced the triazolotriazine core structure with two different heterocyclic cores. One of these, the one deriving from [1,2,4] triazolo [1,5-c] pyrimidine, appears to be particularly effective and selected analogs from this series have been shown to be orally active in a mouse catalepsy model of Parkinson's disease. |
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