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Substituted tetrazoles as multipurpose screening compounds.

Nicole Rüger1, Georg Michael Fassauer1, Christian Bock1

  • 1Institute of Pharmacy, Ernst-Moritz-Arndt-University Greifswald, Friedrich-Ludwig-Jahn-Str. 17, 17487, Greifswald, Germany.

Molecular Diversity
|December 29, 2016
PubMed
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This study synthesizes novel polydentate tetrazole compounds for drug discovery. These compounds, rich in under-represented tetrazole derivatives, offer potential for targeting difficult or previously undruggable proteins.

Area of Science:

  • Medicinal Chemistry
  • Organic Synthesis
  • Drug Discovery

Background:

  • Tetrazoles are versatile heterocycles acting as aromatic platforms and interaction motifs.
  • Tetrazole derivatives can chelate metal ions, exhibiting diverse binding modes.
  • Previous work showed tetrazole-hydrazide fragments are effective for discovering selective screening hits.

Purpose of the Study:

  • To synthesize and characterize novel polydentate tetrazole-containing screening compounds.
  • To expand the chemical space of tetrazole derivatives available for drug discovery.
  • To deposit these compounds into a multipurpose screening library within the EU-OPENSCREEN network.

Main Methods:

  • Synthesis of tetrazole-containing compounds and their precursors.
Keywords:
High-throughput screeningHydrazidesHydrazonesMetal complexing agentsOpen access data bankTargeted library

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  • Characterization of the synthesized compounds.
  • Deposition of pure compounds into a screening library.
  • Main Results:

    • Successful synthesis and characterization of new polydentate tetrazole screening compounds.
    • Availability of under-represented tetrazole derivatives for screening.
    • Compounds are deposited in a multipurpose screening library.

    Conclusions:

    • The synthesized tetrazole compounds are well-characterized and suitable for drug discovery programs.
    • These novel compounds can aid in targeting multiple or previously undruggable protein targets.
    • The inclusion of under-represented tetrazole derivatives enriches the screening library.