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

Michael Brands1, Jens-Kerim Ergüden, Kentaro Hashimoto

  • 1BAYER HealthCare AG, Business Group Pharma, Research & Development, D-42096 Wuppertal, Germany. michael.brands@bayerhealthcare.com

Bioorganic & Medicinal Chemistry Letters
|August 9, 2005
PubMed
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Researchers discovered novel indole-based inhibitors for endothelin-converting enzyme (ECE). Systematic chemical optimization yielded potent compounds with low-nanomolar activity, advancing ECE inhibitor development.

Area of Science:

  • Medicinal Chemistry
  • Drug Discovery
  • Biochemistry

Background:

  • Endothelin-converting enzyme (ECE) plays a critical role in cardiovascular and nervous systems.
  • Developing selective ECE inhibitors is a key therapeutic goal.

Purpose of the Study:

  • To identify and optimize novel indole-based inhibitors of endothelin-converting enzyme (ECE).

Main Methods:

  • High-throughput screening (HTS) was employed to identify initial hit compounds.
  • Classical and solid-phase chemistry techniques were used for systematic structure optimization.
  • In vitro assays were performed to evaluate inhibitory activity against ECE.

Main Results:

  • A novel class of indole-based compounds targeting ECE was discovered.

Related Experiment Videos

  • Optimization efforts focused on the 2-position of the indole skeleton.
  • Compounds featuring a bisarylamide side chain demonstrated potent low-nanomolar activity against ECE.

    • Conclusions:

    • The identified indole-based compounds represent a promising new class of ECE inhibitors.
    • Further development of these optimized compounds could lead to novel therapeutic agents.
    • This study highlights the success of integrated HTS and chemical optimization in drug discovery.