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Macrocyclization strategy for improving candidate profiles in medicinal chemistry.

Om Darlami1, Rabin Pun1, Sung-Hoon Ahn2

  • 1College of Pharmacy, Gachon University, Hambakmoe-ro 191, Yeunsu-gu, Incheon, 21935, Republic of Korea.

European Journal of Medicinal Chemistry
|May 16, 2024
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Summary

Macrocycles, cyclic compounds with 12+ members, offer structural diversity for high-affinity drug targets. This review details macrocyclization strategies for optimizing drug properties and efficacy in medicinal chemistry.

Keywords:
MacrocycleMacrocyclizationPharmacokineticsPotencySelectivityhERG

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Area of Science:

  • Medicinal Chemistry
  • Drug Discovery
  • Organic Chemistry

Background:

  • Macrocycles are cyclic compounds with 12 or more members.
  • They offer structural diversity and high affinity/selectivity for challenging drug targets.
  • Macrocyclization optimizes drug-like properties, bioavailability, and permeability.

Purpose of the Study:

  • To provide a detailed case study on macrocyclization applications in medicinal chemistry over the past 5 years.
  • To illustrate the strategic value of macrocyclization in modern drug discovery.
  • To highlight the optimization of macrocycles from acyclic precursors for improved efficacy.

Main Methods:

  • Review of recent literature (past 5 years) on macrocyclization strategies.
  • Analysis of case studies involving the transition from acyclic compounds to macrocyclic drugs.
  • Evaluation of methods for optimizing macrocycle efficacy and drug-like properties.

Main Results:

  • Macrocyclization enables targeting of previously intractable biological targets.
  • The process allows for fine-tuning of pharmacokinetic and pharmacodynamic properties.
  • Successful optimization leads to enhanced efficacy and improved drug-like characteristics.

Conclusions:

  • Macrocyclization is a key innovation in medicinal chemistry for developing novel therapeutics.
  • It provides a powerful strategy for addressing complex drug targets.
  • The application of macrocyclization significantly advances contemporary drug discovery efforts.