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Published on: September 28, 2022
Macrocyclic drugs and synthetic methodologies toward macrocycles.
1Department of Pharmaceutical Sciences, The Daniel K. Inouye College of Pharmacy, University of Hawai'i at Hilo, 34 Rainbow Drive, Hilo, HI 96720, USA.
Molecules (Basel, Switzerland)
|May 28, 2013
Summary
Macrocyclic drugs are vital in medicine. This review covers their synthesis, therapeutic potential, and common synthetic methods for creating these complex molecules.
Area of Science:
- Medicinal Chemistry
- Organic Synthesis
Background:
- Macrocyclic scaffolds are prevalent in bioactive natural products and pharmaceuticals.
- Synthesizing macrocycles is a critical and challenging aspect of natural product synthesis.
Purpose of the Study:
- To review current macrocyclic drugs.
- To highlight the therapeutic potential of macrocycles.
- To outline synthetic methodologies for macrocycle construction.
Main Methods:
- Overview of established macrocyclization techniques.
- Discussion of transition metal-catalyzed cross-coupling.
- Inclusion of ring-closing metathesis and click reactions.
Main Results:
- Compilation of commonly used macrocyclic drugs.
- Identification of various synthetic routes for macrocycle formation.
- Examples of synthesized natural products and drug-like macrocycles.
Conclusions:
- Macrocycles represent an important, yet underexplored, class of therapeutic agents.
- Advances in synthetic methodologies facilitate the construction of complex macrocyclic structures.
- Further exploration of macrocyclic drugs is warranted for therapeutic advancement.
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