A nonneglectable stereochemical factor in drug development: Atropisomerism

Chirality is one of the key factors affecting the medicinal efficacy of compounds. In addition to central chirality, sterically hindered chiral axes commonly appear in drugs and the resulting chirality is known as atropisomerism. With developments in medicinal chemistry, atropisomerism has attracted...

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Bibliographic Details
Published inChirality (New York, N.Y.) Vol. 34; no. 10; pp. 1355 - 1370
Main Authors Yang, Ya‐Dong, Yang, Bei‐Bei, Li, Li
Format Journal Article
LanguageEnglish
Published Chichester Wiley Subscription Services, Inc 01.10.2022
Subjects
atropisomerism
axial chirality
Biological activity
chiral drug
Chirality
configuration assignment
Drug development
Drugs
Pharmacokinetics
R&D
Research & development
Side effects
stereochemistry
Toxicity
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Summary:Chirality is one of the key factors affecting the medicinal efficacy of compounds. In addition to central chirality, sterically hindered chiral axes commonly appear in drugs and the resulting chirality is known as atropisomerism. With developments in medicinal chemistry, atropisomerism has attracted increasing attention. This review discusses the classification, biological activity, pharmacokinetics, toxicity and side effects of atropisomers, and can serve as a reference in the research and development of potential chiral drugs.
Bibliography:ObjectType-Article-2
SourceType-Scholarly Journals-1
ObjectType-Feature-3
content type line 23
ObjectType-Review-1
ISSN:0899-0042
1520-636X
DOI:10.1002/chir.23497