Peer-reviewed veterinary case report
Optimization of arylindenopyrimidines as potent adenosine A(2A)/A(1) antagonists.
- Journal:
- Bioorganic & medicinal chemistry letters
- Year:
- 2010
- Authors:
- Shook, Brian C et al.
- Affiliation:
- Johnson & Johnson Pharmaceutical Research and Development · United States
Abstract
Two reactive metabolites were identified in vivo for the dual A(2A)/A(1) receptor antagonist 1. Two strategies were implemented to successfully mitigate the metabolic liabilities associated with 1. Optimization of the arylindenopyrimidines led to a number of amide, ether, and amino analogs having comparable in vitro and in vivo activity.
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Search related cases →Original publication: https://pubmed.ncbi.nlm.nih.gov/20338760/