2-(2-Furanyl)-7-phenyl[1,2,4]triazolo[1,5-c]pyrimidin-5-amine analogs: highly potent, orally active, adenosine A2A antagonists. Part 1

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 A(2A) receptor antagonism. Several compounds displayed oral activity at 3 mg/kg in a...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2005-08, Vol.15 (16), p.3670-3674
Main Authors: Matasi, Julius J, Caldwell, John P, Zhang, Hongtao, Fawzi, Ahmad, Cohen-Williams, Mary E, Varty, Geoffrey B, Tulshian, Deen B
Format: Article
Language:English
Subjects:
Adenosine A2 Receptor Antagonists
Administration, Oral
Animals
Catalepsy - drug therapy
Disease Models, Animal
Drug Evaluation, Preclinical
Male
Molecular Structure
Pyrimidines - chemistry
Pyrimidines - classification
Pyrimidines - pharmacology
Pyrimidines - therapeutic use
Rats
Structure-Activity Relationship
Triazoles - chemistry
Triazoles - pharmacology
Triazoles - therapeutic use
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Summary: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 A(2A) 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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2005.05.086