Discovery of N-(3-{4-[(3-Fluorobenzyl)oxy]phenoxy}propyl)-2-pyridin-4-ylacetamide as a Potent and Selective Reverse NCX Inhibitor
| Autor: | Shuichi Sakamoto, Takahiro Kuramochi, Hiroyoshi Yamada, Akio Kakefuda, Takashi Ogiyama, Taku Taguchi |
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| Rok vydání: | 2005 |
| Předmět: |
Magnetic Resonance Spectroscopy
Pyridines Chemistry Transporter General Chemistry General Medicine Spectrometry Mass Fast Atom Bombardment Pharmacology Inhibitory postsynaptic potential medicine.disease Sodium-Calcium Exchanger Heart failure Acetamides Drug Discovery medicine Anti arrhythmic Calcium overload IC50 |
| Zdroj: | Chemical and Pharmaceutical Bulletin. 53:1043-1047 |
| ISSN: | 1347-5223 0009-2363 |
| DOI: | 10.1248/cpb.53.1043 |
| Popis: | 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 IC50 value of 0.085 microM against reverse NCX. |
| Databáze: | OpenAIRE |
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