Peer-reviewed veterinary case report
Synthesis of alkyne derivatives of a novel triazolopyrazine as A(2A) adenosine receptor antagonists.
- Journal:
- Bioorganic & medicinal chemistry letters
- Year:
- 2005
- Authors:
- Yao, Gang et al.
- Affiliation:
- Departments of Medicinal Chemistry and Pharmacology · United States
- Species:
- rodent
Abstract
A novel [1,2,4]triazolo[1,5-a]pyrazine core was synthesized and coupled with terminal acetylenes. The structure-activity relationship of the alkynes from this novel template was studied for their in vitro and in vivo adenosine A(2A) receptor antagonism. Selected compounds from this series were shown to have potent in vitro and in vivo activities against adenosine A(2A) receptor. Compound 12, in particular, was found to be orally active at 3mg/kg in both a mouse catalepsy model and a 6-hydroxydopamine-lesioned rat model.
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Search related cases →Original publication: https://pubmed.ncbi.nlm.nih.gov/15664803/