Discovery of N-(3-{4-[(3-Fluorobenzyl)oxy]phenoxy}propyl)-2-pyridin-4-ylacetamide as a Potent and Selective Reverse NCX Inhibitor

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概要

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• In the setting of heart failure and myocardial ischemia-reperfusion, the sodium-calcium exchanger (NCX) can lead to calcium overload, which is responsible for contractile dysfunction and arrhythmia. NCX is an attractive target for treatment in heart failure and myocardial ischemia-reperfusion. We have designed and synthesized a series of benzyloxyphenyl derivatives based on compound 3. These derivatives have been evaluated for their inhibitory activity against both the reverse and forward modes of NCX. We have discovered a novel potent and selective reverse NCX inhibitor (12) with an IC_<50> value of 0.085μM against reverse NCX.

• 公益社団法人日本薬学会の論文
• 2005-08-01

著者

• Kuramochi Takahiro

  Drug Discovery Research Astellas Pharma Inc.

• Kakefuda Akio

  Drug Discovery Research Astellas Pharma Inc.

• YAMADA Hiroyoshi

  Drug Discovery Research, Astellas Pharma Inc.

• OGIYAMA Takashi

  Drug Discovery Research, Astellas Pharma Inc.

• TAGUCHI Taku

  QA & RA and Pharmacovigilance, Astellas Pharma Inc.

• SAKAMOTO Shuichi

  I Technology, Astellas Pharma Inc.

• Sakamoto Shuichi

  I Technology Astellas Pharma Inc.

• Ogiyama Takashi

  Drug Discovery Research Astellas Pharma Inc.

• Taguchi Taku

  Qa & Ra And Pharmacovigilance Astellas Pharma Inc.

• Yamada Hiroyoshi

  Drug Discovery Research Astellas Pharma Inc.

関連論文

• Discovery of N-(3-{4-[(3-Fluorobenzyl)oxy]phenoxy}propyl)-2-pyridin-4-ylacetamide as a Potent and Selective Reverse NCX Inhibitor

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