Novel, selective indole-based ECE inhibitors: lead optimization via solid-phase and classical synthesis

Bioorganic & Medicinal Chemistry Letters
Michael BrandsStefan Weigand


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.


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