Discovery of N-(3-{4-[(3-Fluorobenzyl)oxy]phenoxy}propyl)-2-pyridin-4-ylacetamide as a Potent and Selective Reverse NCX Inhibitor
-
- 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.
Search this article
Abstract
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 μM against reverse NCX.
Journal
-
- Chemical and Pharmaceutical Bulletin
-
Chemical and Pharmaceutical Bulletin 53 (8), 1043-1047, 2005
The Pharmaceutical Society of Japan
- Tweet
Details 詳細情報について
-
- CRID
- 1390001204170828800
-
- NII Article ID
- 10016656235
-
- NII Book ID
- AA00602100
-
- ISSN
- 13475223
- 00092363
-
- NDL BIB ID
- 7373216
-
- PubMed
- 16079546
-
- Text Lang
- en
-
- Data Source
-
- JaLC
- NDL
- Crossref
- PubMed
- CiNii Articles
-
- Abstract License Flag
- Disallowed
