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Novel heterocyclic thyromimetics. Part 2.

Helmut Haning1, Ulrich Mueller, Gunter Schmidt

  • 1Bayer HealthCare AG, Bayer Schering Pharma Global Drug Discovery, D-42096 Wuppertal, Germany. Helmut.Haning@bayerhealthcare.com

Bioorganic & Medicinal Chemistry Letters
|May 15, 2007
PubMed
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Novel heterocyclic compounds acting as thyroid hormone receptor agonists were developed. These thyromimetics, featuring benzofurans or sulfur heterocycles, show potent activity but lack thyroid hormone receptor isoform selectivity in vitro and in vivo.

Area of Science:

  • Medicinal Chemistry
  • Endocrinology
  • Drug Discovery

Background:

  • Thyroid hormones are crucial for metabolism and development.
  • Thyroid hormone receptor (THR) agonists are sought for therapeutic applications.
  • Existing thyromimetics often face challenges with selectivity and side effects.

Purpose of the Study:

  • To design and synthesize novel heterocyclic thyromimetics.
  • To evaluate the agonist activity of these compounds at thyroid hormone receptors.
  • To investigate the structure-activity relationships (SAR) and isoform selectivity.

Main Methods:

  • Synthesis of novel benzofuran and sulfur-containing heterocyclic compounds.
  • In vitro assays including transient transfection assays for THR isoform selectivity.

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  • In vivo studies to confirm findings from in vitro assays.

    • Main Results:

    • Identification of potent agonist activity in both benzofuran and sulfur-containing heterocyclic series.
    • Structure-activity relationship trends were consistent with known thyromimetics.
    • Lack of thyroid hormone receptor isoform selectivity was confirmed in both in vitro and in vivo models.

    Conclusions:

    • Novel heterocyclic scaffolds can yield potent thyroid hormone receptor agonists.
    • These compounds represent a promising starting point for further drug development.
    • The identified compounds lack isoform selectivity, a key consideration for therapeutic development.