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Asymmetric Synthesis, Enantioselective Analysis and Chiral Recognition

A special issue of Molecules (ISSN 1420-3049).

Deadline for manuscript submissions: closed (31 July 2020) | Viewed by 4667

Special Issue Editor


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Guest Editor
Chirality Group, Biomedical Science Program, School of Science, Faculty of Science and Technology, University of Canberra, Canberra, ACT 2601, Australia
Interests: chirality; enantioselective nano chromatography; asymmetric catalysis; chiral analysis
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

The importance of chirality and its medical impact has steadily increased in the last decades and it is currently a central hot topic in organic and pharmaceutical chemistry, and in particular, the development of new drugs. Recently the first deuterated chiral drug was approved by US Food and Drug Administration (FDA) for therapeutic use as a long acting drug used in the treatment of chorea in Huntington’s disease (HD). Austedo or deutetrabenazine is the deuterated version of the chiral tetrabenazine drug. To establish that its beneficial therapeutic actions are enantiospecific, a practical total synthetic route was developed to yield separate enantiomeric forms, allowing their chemical and pharmacological characterization. The latter is a mandatory FDA requirement for all new drugs where stereochemistry is involved. Similarly, many chiral drugs in the market involve asymmetric or enantioselective synthesis, chiral or enantioselective analysis, and the understanding of the chiral recognition mechanism.
This Special Issue aims to deal with all sorts of chirality, from asymmetric/enantioselective synthesis to chiral analysis with an understanding of the chiral recognition mechanism. Theoretical, fundamental, practical studies in multidisciplinary approaches are all welcome for consideration. Contributions may be in the form of original research or review articles covering the broad scope of chirality, its impact, and applications.

Prof. Dr. Ashraf Ghanem
Guest Editor

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Molecules is an international peer-reviewed open access semimonthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2700 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • chirality
  • enantioselective chromatography
  • chiral separation
  • chiral recognition
  • asymmetric synthesis
  • asymmetric catalysis
  • chiral recognition

Published Papers (1 paper)

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Review

19 pages, 3894 KiB  
Review
Chiral Aspects of Local Anesthetics
by Ružena Čižmáriková, Jozef Čižmárik, Jindra Valentová, Ladislav Habala and Mário Markuliak
Molecules 2020, 25(12), 2738; https://doi.org/10.3390/molecules25122738 - 12 Jun 2020
Cited by 15 | Viewed by 4202
Abstract
Thanks to the progress made in chemical technology (particularly in the methodologies of stereoselective syntheses and analyses) along with regulatory measures, the number of new chiral drugs registered in the form of pure enantiomers has increased over the past decade. In addition, the [...] Read more.
Thanks to the progress made in chemical technology (particularly in the methodologies of stereoselective syntheses and analyses) along with regulatory measures, the number of new chiral drugs registered in the form of pure enantiomers has increased over the past decade. In addition, the pharmacological and pharmacokinetic properties of the individual enantiomers of already-introduced racemic drugs are being re-examined. The use of the pure enantiomer of a drug that has been used to date in the form of a racemate is called a “chiral switch”. A re-examination of the properties of the pure enantiomers of racemates has taken place for local anesthetics, which represent a group of drugs which have long been used. Differences in (R) and (S)-enantiomers were found in terms of pharmacodynamic and pharmacokinetic activity as well as in toxicity. Levobupivacaine and robivacaine were introduced into practice as pure (S)-(−)-enantiomers, exhibiting more favorable properties than their (R)-(+)-stereoisomers or racemates. This overview focuses on the influence of chirality on the pharmacological and toxicological activity of local anesthetics as well as on individual HPLC and capillary electrophoresis (CE) methods used for enantioseparation and the pharmacokinetic study of individual local anesthetics with a chiral center. Full article
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