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Related Experiment Videos

Thrombin inhibitors based on [5,5] trans-fused indane lactams.

M Pass1, S Abu-Rabie, A Baxter

  • 1Glaxo Wellcome Research and Development, Stevenage, Herts, United Kingdom. mp8073@glaxowellcome.co.uk

Bioorganic & Medicinal Chemistry Letters
|July 9, 1999
PubMed
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Researchers synthesized novel trans-fused lactams with an indane core. Compound 19 demonstrated improved plasma stability and significant in vitro anticoagulant effects, outperforming its lactone analog.

Area of Science:

  • Medicinal Chemistry
  • Organic Synthesis
  • Pharmacology

Background:

  • Lactam and lactone structures are common in biologically active molecules.
  • Indane derivatives have shown diverse pharmacological properties.
  • Developing stable anticoagulant agents remains a significant therapeutic challenge.

Purpose of the Study:

  • To synthesize and characterize novel trans-fused lactam compounds incorporating the indane nucleus.
  • To evaluate the plasma stability and in vitro anticoagulant activity of these novel lactams.
  • To compare the properties of the synthesized lactams with their corresponding lactone analogs.

Main Methods:

  • Multi-step organic synthesis to prepare a series of trans-fused lactams.
  • Characterization of synthesized compounds using spectroscopic techniques.

Related Experiment Videos

  • In vitro assays to assess plasma stability and anticoagulant activity (e.g., Prothrombin Time, Activated Partial Thromboplastin Time).
  • Main Results:

    • Successful synthesis of a series of trans-fused lactams containing the indane moiety.
    • Compound 19 exhibited significantly enhanced plasma stability compared to its lactone counterpart.
    • Compound 19 demonstrated appreciable in vitro anticoagulant activity.

    Conclusions:

    • Trans-fused lactams based on the indane nucleus represent a promising class of compounds.
    • The enhanced plasma stability of Compound 19 suggests potential for improved pharmacokinetic profiles.
    • These findings warrant further investigation into the therapeutic potential of these novel lactam derivatives as anticoagulants.