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Molecules
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Chiral Drugs
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Chiral Drugs

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: closed (10 May 2016) | Viewed by 19959

Special Issue Editor

Prof. Dr. Claudio Villani

E-Mail Website
Guest Editor
Dipartimento di Chimica e Tecnologie del Farmaco, Universita degli Studi di Roma La Sapienza, Rome, Italy
Interests: chirality; organic stereochemistry; stereodynamics; separation science; mass spectrometry
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Chirality in drug molecules has a profound impact in several aspects of their design, research, and development.

Enantiomers have identical physical and chemical properties in an achiral environment, but they usually display different biological activities because they can interact differently with natural targets like receptors and enzymes.

Recent more stringent policies from drug regulatory agencies worldwide, together with improvements in the synthetic and analytical technologies for the production and control of enantiomerically pure compounds, have changed the approach to chiral drugs both in academia and pharmaceutical industry.

Improved, efficient and scalable asymmetric synthesis, resolution processes, fast and precise enantioselective chromatographic separations at analytical scales and cost effective separations at preparative levels, experimental and theoretical advances in chiroptical techniques for the absolute configuration determination are just a few examples of the large body of attributes of chiral drugs.

This Special Issue is intended to give an updated overview of modern synthetic, analytical and spectroscopic methods to produce and characterize new chiral drugs.

Prof. Claudio Villani
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

  • asymmetric synthesis
  • resolution techniques
  • chirality in natural products
  • enantioselective analysis
  • enantioselective chromatography
  • chiroptical spectroscopy
  • absolute configuration
  • chiral recognition
  • chirality and pharmacokinetics
  • chirality and pharmacodynamics
  • chirality and clinical pharmacology
  • chirality and regulatory aspects

Published Papers (3 papers)

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Research

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2390 KiB  
Article
Novel Enantiopure Sigma Receptor Modulators: Quick (Semi-)Preparative Chiral Resolution via HPLC and Absolute Configuration Assignment
by Marta Rui, Annamaria Marra, Vittorio Pace, Markus Juza, Daniela Rossi and Simona Collina
Molecules 2016, 21(9), 1210; https://doi.org/10.3390/molecules21091210 - 10 Sep 2016
Cited by 7 | Viewed by 5009
Abstract
The identification of novel pan-sigma receptor (SR) modulators, potentially useful in cancer treatment, represents a new goal of our research. Here, we report on the preparation of novel chiral compounds characterized by a 3-C alkyl chain bridging an aromatic portion to a 4-benzyl-piperidine [...] Read more.
The identification of novel pan-sigma receptor (SR) modulators, potentially useful in cancer treatment, represents a new goal of our research. Here, we report on the preparation of novel chiral compounds characterized by a 3-C alkyl chain bridging an aromatic portion to a 4-benzyl-piperidine moiety. All of the studied compounds have been prepared both in racemic and enantiomerically-pure form, with the final aim to address the role of chirality in the SR interaction. To isolate and characterize enantiomeric compounds, high-performance liquid chromatography (HPLC) procedures were set up. A systematic analytical screening, involving several combinations of chiral stationary and mobile phases, allowed us to optimize the analytical resolution and to set up the (semi-)preparative chromatographic conditions. Applying the optimized procedure, the enantiomeric resolution of the studied compounds was successfully achieved, obtaining all of the compounds with an enantiomeric excess higher than 95%. Lastly, the absolute configuration has been empirically assigned to enantiopure compounds, combining the electronic circular dichroism (ECD) technique to the elution order study. Full article
(This article belongs to the Special Issue Chiral Drugs)
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Review

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962 KiB  
Review
Determination of the Absolute Configurations of Chiral Drugs Using Chiroptical Spectroscopy
by Prasad L. Polavarapu
Molecules 2016, 21(8), 1056; https://doi.org/10.3390/molecules21081056 - 12 Aug 2016
Cited by 35 | Viewed by 6582
Abstract
Chiroptical spectroscopy has emerged as a promising tool for the determination of absolute configurations and predominant conformations of chiral molecules in academic laboratories. This promise has led to the adaption of chiroptical spectroscopic methods as valuable tools in chiral drug discovery research programs [...] Read more.
Chiroptical spectroscopy has emerged as a promising tool for the determination of absolute configurations and predominant conformations of chiral molecules in academic laboratories. This promise has led to the adaption of chiroptical spectroscopic methods as valuable tools in chiral drug discovery research programs of the pharmaceutical industry. Most major pharmaceutical companies have invested in in-house chiroptical spectroscopy applications and reported successful outcomes. In the context of continuously increasing applications of chiroptical spectroscopy for chiral molecular structure determination, a review of recent developments and applications for chiral drugs is presented in this manuscript. Full article
(This article belongs to the Special Issue Chiral Drugs)
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2211 KiB  
Review
Focus on Chirality of HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors
by Valeria Famiglini and Romano Silvestri
Molecules 2016, 21(2), 221; https://doi.org/10.3390/molecules21020221 - 16 Feb 2016
Cited by 21 | Viewed by 7634
Abstract
Chiral HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) are of great interest since one enantiomer is often more potent than the corresponding counterpart against the HIV-1 wild type (WT) and the HIV-1 drug resistant mutant strains. This review exemplifies the various studies made to [...] Read more.
Chiral HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) are of great interest since one enantiomer is often more potent than the corresponding counterpart against the HIV-1 wild type (WT) and the HIV-1 drug resistant mutant strains. This review exemplifies the various studies made to investigate the effect of chirality on the antiretroviral activity of top HIV-1 NNRTI compounds, such as nevirapine (NVP), efavirenz (EFV), alkynyl- and alkenylquinazolinone DuPont compounds (DPC), diarylpyrimidine (DAPY), dihydroalkyloxybenzyloxopyrimidine (DABO), phenethylthiazolylthiourea (PETT), indolylarylsulfone (IAS), arylphosphoindole (API) and trifluoromethylated indole (TFMI) The chiral separation, the enantiosynthesis, along with the biological properties of these HIV-1 NNRTIs, are discussed. Full article
(This article belongs to the Special Issue Chiral Drugs)
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