降低一系列 4-杂环芳酰胺 FMS 抑制剂中的离子通道活性。
Reducing ion channel activity in a series of 4-heterocyclic arylamide FMS inhibitors.
机构信息
Johnson & Johnson Pharmaceutical Research & Development, Spring House, PA 19477, USA.
出版信息
Bioorg Med Chem Lett. 2010 Jul 1;20(13):3925-9. doi: 10.1016/j.bmcl.2010.05.013. Epub 2010 May 12.
PMID:20570147
Abstract
During efforts to improve the bioavailability of FMS kinase inhibitors 1 and 2, a series of saturated and aromatic 4-heterocycles of reduced basicity were prepared and evaluated in an attempt to also improve the cardiovascular safety profile over lead arylamide 1, which possessed ion channel activity. The resultant compounds retained excellent potency and exhibited diminished ion channel activity.
摘要
在提高 FMS 激酶抑制剂 1 和 2 的生物利用度的努力中，我们合成了一系列饱和的和芳香的、碱性降低的 4-杂环化合物，同时尝试改善先导芳基酰胺 1 的心血管安全性，因为它具有离子通道活性。得到的化合物保持了优异的效力，同时表现出降低的离子通道活性。
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