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05:15
Solid-phase Synthesis of [4.4] Spirocyclic Oximes
Published on: February 6, 2019
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A nonneglectable stereochemical factor in drug development: Atropisomerism
Ya-Dong Yang1, Bei-Bei Yang1, Li Li1
1Beijing Key Laboratory of Active Substances Discovery and Druggability Evaluation, Institute of Materia Medica, Chinese Academy of Medical Sciences, Peking Union Medical College, Beijing, China.
Chirality
|July 29, 2022
Summary
Chirality impacts drug effectiveness, with atropisomerism gaining focus in medicinal chemistry. This review covers atropisomer properties, aiding chiral drug development.
Area of Science:
- Medicinal Chemistry
- Organic Chemistry
- Pharmacology
Background:
- Chirality is crucial for drug efficacy.
- Atropisomerism, arising from sterically hindered chiral axes, is increasingly recognized in pharmaceuticals.
- Understanding atropisomers is vital for developing safer and more effective medicines.
Purpose of the Study:
- To provide a comprehensive overview of atropisomerism in medicinal chemistry.
- To discuss the classification, biological activity, pharmacokinetics, toxicity, and side effects of atropisomers.
- To serve as a reference for the research and development of chiral drugs.
Main Methods:
- Literature review of atropisomerism in drug development.
- Analysis of published data on atropisomer classification and properties.
- Synthesis of information on biological activity, pharmacokinetics, and toxicity.
Main Results:
- Atropisomerism is a significant source of chirality in drug molecules.
- Detailed discussion on the various aspects of atropisomer pharmacology and toxicology.
- Identification of atropisomers as key targets for chiral drug design.
Conclusions:
- Atropisomerism is an important consideration in modern drug discovery.
- This review consolidates current knowledge on atropisomers, facilitating future research.
- Further investigation into atropisomers will enhance the development of novel chiral therapeutics.
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