| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1379568 | Bioorganic & Medicinal Chemistry Letters | 2005 | 5 Pages |
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.
Graphical abstractA 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.Figure optionsDownload full-size imageDownload as PowerPoint slide
