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Drug Discovery: Overview01:26

Drug Discovery: Overview

Drug discovery is a multifaceted process involving extensive screening, testing, and optimization of lead compounds to identify potential new drugs for therapeutic use. It combines several approaches, including screening large numbers of natural products, chemical modification of known active molecules, identification of new drug targets, and rational design based on biological mechanisms and drug-receptor structure. These approaches are carried out in both academic research laboratories and...

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Updated: Jun 14, 2026

A Method for Selecting Structure-switching Aptamers Applied to a Colorimetric Gold Nanoparticle Assay
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Medium-Sized Ring Expansion Strategies: Enhancing Small-Molecule Library Development.

Hwiyeong Lee1, Jonghoon Kim2, Minseob Koh1

  • 1Department of Chemistry and Chemistry Institute for Functional Materials, Pusan National University, Busan 46241, Republic of Korea.

Molecules (Basel, Switzerland)
|April 13, 2024
PubMed
Summary
This summary is machine-generated.

Synthesizing medium-sized rings is crucial for drug discovery, enabling the targeting of difficult proteins. This review explores innovative synthetic strategies to overcome challenges and expand chemical diversity for new medicines.

Keywords:
bioactive compound discoverydiversity-oriented synthesismedium-sized ring synthesisnatural product mimicsring-expansion reactions

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Area of Science:

  • Medicinal Chemistry
  • Organic Synthesis

Background:

  • Medium-sized rings are vital scaffolds in drug discovery for targeting challenging proteins.
  • Their structural complexity and diversity offer unique opportunities for novel therapeutic agents.
  • Traditional synthesis methods face challenges like transannular strain and limited flexibility.

Purpose of the Study:

  • To review current strategies for synthesizing medium-sized rings.
  • To highlight innovative synthetic methodologies, such as ring-expansion reactions.
  • To underscore the importance of medium-sized rings in expanding chemical space for drug discovery.

Main Methods:

  • Overview of established and emerging synthetic routes for medium-sized rings.
  • Emphasis on ring-expansion reactions as a key strategy.
  • Discussion of challenges associated with synthesizing these complex structures.

Main Results:

  • Identification of key synthetic challenges, including transannular strain.
  • Showcasing of innovative approaches like ring-expansion reactions.
  • Demonstration of how medium-sized rings enhance chemical diversity.

Conclusions:

  • Medium-sized rings are essential for developing novel therapeutics against 'undruggable' targets.
  • Innovative synthetic strategies are crucial for overcoming synthesis challenges.
  • These compounds significantly contribute to diversifying the chemical space in drug discovery.