866826-97-3Relevant academic research and scientific papers
Novel, selective indole-based ECE inhibitors: Lead optimization via solid-phase and classical synthesis
Brands, Michael,Ergueden, Jens-Kerim,Hashimoto, Kentaro,Heimbach, Dirk,Schroeder, Christian,Siegel, Stephan,Stasch, Johannes-Peter,Weigand, Stefan
, p. 4201 - 4205 (2007/10/03)
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.
