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Synthesis and structure-activity relationships of benzyloxyphenyl derivatives as a novel class of NCX inhibitors: effects on heart failure.

Abstract：

:In the context of heart failure and myocardial ischemia reperfusion, the activity of the sodium-calcium exchanger can lead to calcium overload, which in turn can lead to contractile dysfunction and arrhythmia. Therefore, NCX is an attractive target for treatment of heart failure and myocardial ischemia reperfusion. We have designed and synthesized a series of benzyloxyphenyl derivatives as potential NCX inhibitors, based on compound 4. These derivatives have been evaluated for their inhibitory activity against both the reverse and forward modes of NCX, and two novel potent NCX inhibitors (7i, 10a) were discovered. Compound 7i was evaluated for its efficacy on ouabain-induced tonotropy and arrhythmia in a heart-failure model.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Kuramochi T,Kakefuda A,Yamada H,Ogiyama T,Taguchi T,Sakamoto S

doi

10.1016/j.bmc.2004.10.048

subject

Has Abstract

pub_date

2005-02-01 00:00:00

pages

725-34

issue

3

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(04)00851-X

journal_volume

13

pub_type

杂志文章

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