Bioorganic and Medicinal Chemistry Letters p. 3670 - 3674 (2005)
Update date:2022-08-05
Topics:
Matasi, Julius J.
Caldwell, John P.
Zhang, Hongtao
Fawzi, Ahmad
Cohen-Williams, Mary E.
Varty, Geoffrey B.
Tulshian, Deen B.
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 3 mg/kg in a rat catalepsy model. Specifically, compound 8g displayed an excellent in vitro profile, as well as a highly promising in vivo profile.
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