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 ,
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.
