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Cited by 1,224Analytical Chemistry and ChromatographyChemistry and Stereochemistry StudiesMolecular spectroscopy and chirality

The DOI matches its Crossref record; 72 of the 84 references it cites were found in a registry or an index.

Chiral Drugs. An Overview

Open access
Laboratory of Toxicology, Faculty of Pharmacy, University of Paris 5, 4 avenue de l'Observatoire, 75006 Paris, France., Chuong, Pham-Huy, Nguyen, Lien Ai, Department of Pharmacy, Lucile Salter Packard Children's Hospital, Stanford University Medical Center, 725 Welch Road, Palo Alto, CA 94304, USA, He, Hua, Department of Analytical Chemistry, China Pharmaceutical University, Nanjing, 210009, China·2006·International Journal of Biomedical Science
DOI 10.59566/ijbs.2006.2085PMC PMC3614593
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Abstract

About more than half of the drugs currently in use are chiral compounds and near 90% of the last ones are marketed as racemates consisting of an equimolar mixture of two enantiomers. Although they have the same chemical structure, most isomers of chiral drugs exhibit marked differences in biological activities such as pharmacology, toxicology, pharmacokinetics, metabolism etc. Some mechanisms of these properties are also explained. Therefore, it is important to promote the chiral separation and analysis of racemic drugs in pharmaceutical industry as well as in clinic in order to eliminate the unwanted isomer from the preparation and to find an optimal treatment and a right therapeutic control for the patient. In this article, we review the nomenclature, pharmacology, toxicology, pharmacokinetics, metabolism etc of some usual chiral drugs as well as their mechanisms. Different techniques used for the chiral separation in pharmaceutical industry as well as in clinical analyses are also examined.

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Crossref · 10.59566/ijbs.2006.2085

Cites

72 of 72 references verified0 citation errors · 0 not checkable

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Figures

Figure 1 H behind the plane of the paper.
Figure 1 H behind the plane of the paper.CC BY · PubMed Central
Figure 2 Easson-Stedman hypothetical interaction between the two enantiomers of a racemic drug with a receptor at the drug binding sites. The three substituents A, B, C of the active enantiomer (left) can interact with three binding sites a, b, c of a receptor by forming three contacts Aa, Bb and Cc, whereas the inactive enantiomer (right) cannot because the contact is insufficient. Note: This figure is in the publication of McConalthy and Owens (47).
Figure 2 Easson-Stedman hypothetical interaction between the two enantiomers of a racemic drug with a receptor at the drug binding sites. The three substituents A, B, C of the active enantiomer (left) can interact with three binding sites a, b, c of a receptor by forming three contacts Aa, Bb and Cc, whereas the inactive enantiomer (right) cannot because the contact is insufficient. Note: This figure is in the publication of McConalthy and Owens (47).CC BY · PubMed Central

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Citations

Cites

Show all 84 references

Research works printed but not linked: 5

  1. [5]Katzung BG The nature of drugs In: Basic and clinical pharmacology 2004 9th New York Lange Medical Books/McGraw Hill 3 5
  2. [12]Ariens EJ Ariens EJ Soudijn W Timmermans PBMWM Stereoselectivity of bioactive agents: general aspects Stereochemistry and Biological activity of Drugs 1983 Oxford Blackwell Scientific 11 33
  3. [16]Stoschitzky K Lindner W Zernig G Racemic beta-blockers-fixed combinations of different drugs Journal of Clinical and Basic Cardiology 1998 1 1 15 19
  4. [24]Industry Overview organised by scientific update. Conferences An international symposium on chirality 5-7 September 1999 Cambridge University, Cambridge, UK http://www.geocities.com/jefferywinkler/bcc.doc
  5. [43]Scott AK Stereoisomers and drug toxicity. The value of single stereoisomer therapy Drug Safety 1993 8 2 149 159 8452656

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Metadata

Authors
Laboratory of Toxicology, F. O. P., Chuong, P.-H., Nguyen, L. A., Department of Pharmacy, L. S. P. C. H., He, H., & Department of Analytical Chemistry, C. P. U.
ORCID
He, Hua
Venue
International Journal of Biomedical Science
Publisher
International Association of Biomedical Sciences
Published
2006-09-15
Volume
2
Issue
2
Pages
85-100
ISSN
  • 1550-9702 (ISSN-L)
  • 1555-2810
DOI
10.59566/ijbs.2006.2085
PMC
PMC3614593
OpenAlex
W4390049991
Cited by
1,224
References
84
Citations by year
2026: 81 · 2025: 105 · 2024: 106 · 2023: 110 · 2022: 132 · 2021: 113 · 2020: 136 · 2019: 120 · 2018: 87 · 2017: 69 · 2016: 81 · 2015: 26 · 2014: 17 · 2013: 11 · 2012: 7
FWCI
1.11
Type
journal article
Language
en
Open access
Licence
cc-by
Locations
  • International Journal of Biomedical Science (publishedVersion)
  • Europe PMC (PubMed Central) (publishedVersion, cc-by)
  • PubMed Central (publishedVersion, cc-by)
  • PubMed (publishedVersion)
  • PubMed
Topics
  • Physical Sciences › Chemistry › Analytical Chemistry › Analytical Chemistry and Chromatography
  • Physical Sciences › Chemistry › Organic Chemistry › Chemistry and Stereochemistry Studies
  • Physical Sciences › Chemistry › Spectroscopy › Molecular spectroscopy and chirality
Keywords
chiral drugs, enantiomers, racemic mixtures, enantiomer separation, pharmaceutical industry

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