Title of article
Novel, selective indole-based ECE inhibitors: Lead optimization via solid-phase and classical synthesis
Author/Authors
Michael Brands، نويسنده , , Jens-Kerim Ergüden، نويسنده , , Kentaro Hashimoto، نويسنده , , Dirk Heimbach، نويسنده , , Christian Schr?der، نويسنده , , Stephan Siegel، نويسنده , , Johannes-Peter Stasch، نويسنده , , Stefan Weigand، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2005
Pages
5
From page
4201
To page
4205
Abstract
A novel class of indole-based endothelin-converting enzyme (ECE) inhibitors was identified by high throughput screening. We report systematic optimization of this compound class by means of classical and solid-phase chemistry. Optimized compounds with a bisarylamide side chain at the 2-position of the indole skeleton exhibit low-nanomolar activity on ECE.
Keywords
ECE inhibitor , Indole , Solid-phase chemistry
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2005
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
795958
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