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

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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Shook BC,Rassnick S,Chakravarty D,Wallace N,Ault M,Crooke J,Barbay JK,Wang A,Leonard K,Powell MT,Alford V,Hall D,Rupert KC,Heintzelman GR,Hansen K,Bullington JL,Scannevin RH,Carroll K,Lampron L,Westover L,Russell

doi

10.1016/j.bmcl.2010.03.024

subject

Has Abstract

pub_date

2010-05-01 00:00:00

pages

2868-71

issue

9

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(10)00345-8

journal_volume

20

pub_type

杂志文章

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