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Bioorg Med Chem Lett. 2010 May 1;20(9):2868-71. doi: 10.1016/j.bmcl.2010.03.024. Epub 2010 Mar 7.

Optimization of arylindenopyrimidines as potent adenosine A(2A)/A(1) antagonists.

Author information

1
Johnson & Johnson Pharmaceutical Research and Development, L.L.C., Welsh and McKean Roads, PO Box 776, Spring House, PA 19477, United States. bshook@its.jnj.com

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.

PMID:
20338760
DOI:
10.1016/j.bmcl.2010.03.024
[Indexed for MEDLINE]

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