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Metformin, a biological and synthetic overview.

Edson D Hernández-Velázquez1, Clara Alba-Betancourt1, Ángel J Alonso-Castro1

  • 1Universidad de Guanajuato, Campus Guanajuato, División de Ciencias Naturales y Exactas, Departamento de Química, Noria Alta S/N, 36050 Guanajuato, Gto., Mexico.

Bioorganic & Medicinal Chemistry Letters
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PubMed
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Metformin, an anti-hyperglycemic drug, evolved from traditional medicine to become a leading type II diabetes treatment. Its history, synthesis, and diverse biological applications are reviewed.

Keywords:
BisguanidinesCyanoguanidineDiabetesGlucoseMetforminSynthesisToxicity

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Area of Science:

  • Pharmacology
  • Endocrinology
  • Medical History

Background:

  • Metformin is a widely prescribed anti-hyperglycemic medication, particularly for type II diabetes.
  • Its origins trace back to traditional use of goat's rue for blood glucose reduction.
  • The drug's widespread adoption followed its synthesis and evolution from early derivatives.

Purpose of the Study:

  • To review and analyze the historical development of metformin.
  • To examine the synthesis pathways and evolution of metformin derivatives.
  • To explore the diverse biological applications of metformin and its related compounds.

Main Methods:

  • Historical literature review of metformin's origins and development.
  • Analysis of early synthesis routes and derivative studies.
  • Compilation and summary of recent research on metformin's biological activities.

Main Results:

  • Metformin's journey from traditional remedies to a key pharmaceutical.
  • Development of synthetic routes and identification of toxic derivatives (e.g., phenformin, buformin).
  • Emerging research highlights metformin's potential beyond diabetes, including cancer and anti-inflammatory uses.

Conclusions:

  • Metformin has a rich history rooted in traditional medicine.
  • The synthesis and study of metformin and its derivatives have led to significant therapeutic advancements.
  • Metformin exhibits a broad spectrum of biological activities, warranting continued research for novel applications.