1229021-36-6Relevant articles and documents
Optimization of arylindenopyrimidines as potent adenosine A2A/A1 antagonists
Shook, Brian C.,Rassnick, Stefanie,Chakravarty, Devraj,Wallace, Nathaniel,Ault, Mark,Crooke, Jeffrey,Barbay, J. Kent,Wang, Aihua,Leonard, Kristi,Powell, Mark T.,Alford, Vernon,Hall, Daniel,Rupert, Kenneth C.,Heintzelman, Geoffrey R.,Hansen, Kristen,Bullington, James L.,Scannevin, Robert H.,Carroll, Karen,Lampron, Lisa,Westover, Lori,Russell, Ronald,Branum, Shawn,Wells, Kenneth,Damon, Sandra,Youells, Scott,Beauchamp, Derek,Li, Xun,Rhodes, Kenneth,Jackson, Paul F.
scheme or table, p. 2868 - 2871 (2010/07/06)
Two reactive metabolites were identified in vivo for the dual A2A/A1 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.
