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Triazolopyrimidines identified as reversible myeloperoxidase inhibitors

Franck Duclos1, Lynn M Abell1, David G Harden1

  • 1Bristol-Myers Squibb Company , P.O. Box 5400 , Princeton , New Jersey 08543-5400 , USA .

Medchemcomm
|August 16, 2018
PubMed

Insights

Researchers identified a reversible inhibitor for myeloperoxidase (MPO), an enzyme linked to chronic diseases. This discovery offers a potential new treatment strategy for conditions like atherosclerosis by targeting MPO activity.

Area of Science:

  • Biochemistry
  • Immunology
  • Pharmacology

Background:

  • Myeloperoxidase (MPO) is an immune enzyme producing hypochlorous acid.
  • Chronic MPO activity contributes to pathological diseases like atherosclerosis.
  • Targeting MPO offers a potential therapeutic strategy for chronic inflammatory conditions.

Purpose of the Study:

  • To identify a reversible inhibitor of myeloperoxidase (MPO).
  • To develop a high-throughput screening protocol for MPO inhibitors.
  • To explore potential treatments for MPO-associated chronic diseases.

Main Methods:

  • Developed a high-throughput screen and triaging protocol.
  • Identified and characterized a novel reversible MPO inhibitor.
  • Utilized biochemical assays to assess inhibitor efficacy.

Main Results:

  • Successfully identified a reversible inhibitor of myeloperoxidase.
  • The inhibitor is 7-(benzyloxy)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-5-amine.
  • Characterization confirmed the inhibitor's reversible binding to MPO.

Conclusions:

  • A novel reversible MPO inhibitor has been identified.
  • This compound represents a potential therapeutic agent for chronic diseases.
  • Further research may validate MPO inhibition for treating atherosclerosis and related conditions.

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