2-(2-Furanyl)-7-phenyl [1, 2, 4] triazolo [1, 5-c] pyrimidin-5-amine analogs: Highly potent, orally active, adenosine A 2A antagonists. Part 1

…, ME Cohen-Williams, GB Varty, DB Tulshian

Index: Matasi, Julius J.; Caldwell, John P.; Zhang, Hongtao; Fawzi, Ahmad; Cohen-Williams, Mary E.; Varty, Geoffrey B.; Tulshian, Deen B. Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 16 p. 3670 - 3674

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Citation Number: 19

Abstract

The structure–activity relationship of this novel class of compounds based on 2-(2-furanyl)-7- phenyl [1, 2, 4]-triazolo [1, 5-c] pyrimidin-5-amine, 1, and its analogs was evaluated for their in vitro and in vivo adenosine A2A receptor antagonism. Several compounds displayed oral activity at 3mg/kg in a rat catalepsy model. Specifically, compound 8g displayed an excellent in vitro profile, as well as a highly promising in vivo profile.

3H-[1, 2, 4]-Triazolo [5, 1-i] purin-5-amine derivatives as adenosine A 2A antagonists

[Silverman, Lisa S.; Caldwell, John P.; Greenlee, William J.; Kiselgof, Eugenia; Matasi, Julius J.; Tulshian, Deen B.; Arik, Leyla; Foster, Carolyn; Bertorelli, Rosalia; Monopoli, Angela; Ongini, Ennio Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 6 p. 1659 - 1662]

3H-[1, 2, 4]-Triazolo [5, 1-i] purin-5-amine derivatives as adenosine A 2A antagonists

2-(2-Furanyl)-7-phenyl [1, 2, 4] triazolo [1, 5-c] pyrimidin-5-amine analogs: Highly potent, orally active, adenosine A 2A antagonists. Part 1

Abstract

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