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

Bioorganic & Medicinal Chemistry Letters
Michael BrandsStefan Weigand

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.

References

Apr 6, 2004·Trends in Pharmacological Sciences·Tomoh Masaki

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Citations

Nov 26, 2009·Beilstein Journal of Organic Chemistry·Mohosin LayekManojit Pal
Aug 5, 2008·Vascular Pharmacology·P D'Orléans-JusteE Simard
Aug 8, 2006·ChemMedChem·Michael BrandsNagahiro H Yoshida
Nov 21, 2019·Anti-cancer Agents in Medicinal Chemistry·Leonard BarasaSabesan Yoganathan

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