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Synthesis and Application of Chiral Ligands and Heterocycles in Pharmacological Studies

A special issue of International Journal of Molecular Sciences (ISSN 1422-0067). This special issue belongs to the section "Molecular Pharmacology".

Deadline for manuscript submissions: 20 November 2025 | Viewed by 607

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Special Issue Information

Dear Colleagues,

We are delighted to announce a call for submissions to a Special Issue of the International Journal of Molecular Sciences on the topic of the synthesis and application of chiral ligands and heterocycles in pharmacological studies.

A variety of approved drug molecules have chiral properties that should be investigated before the molecule can become an API. Usually, one of the enantiomers has more potent biological activity, or the other is not just biologically inactive but can also exhibit harmful effects. We have plenty of examples for both cases, e.g., verapamil, DOPA, ketoprofen, bupivacaine, etc. The synthesis of enantiomerically pure molecules is often expensive and not selective enough; therefore, it is important to investigate new chiral ligands and catalysts in pharmaceutical research. This topic is not only a challenge for pharmaceutical chemists but also presents an obstacle for pharmacologists. We encourage the submission of both original research articles and topical reviews on all aspects of the synthesis and application of chiral ligands and heterocycles in pharmacological studies. All submitted articles will undergo a peer review process.

Prof. Dr. István Szatmári
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. International Journal of Molecular Sciences is an international peer-reviewed open access semimonthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. There is an Article Processing Charge (APC) for publication in this open access journal. For details about the APC please see here. 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

  • nonracemic amino acids
  • enantioselective synthesis
  • chiral catalysis
  • enantiopure bioconjugates
  • electron-rich hydroxyquinoline
  • indole
  • β-carboline
  • bioactive compounds

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Published Papers (1 paper)

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Research

22 pages, 5194 KiB  
Article
Synthesis and Antimicrobial Evaluation of (+)-Neoisopulegol-Based Amino and Thiol Adducts
by Reem Moustafa, Attila Márió Remete, Zsolt Szakonyi, Nikoletta Szemerédi, Gabriella Spengler and Tam Minh Le
Int. J. Mol. Sci. 2025, 26(10), 4791; https://doi.org/10.3390/ijms26104791 - 16 May 2025
Viewed by 205
Abstract
A library of neoisopulegol-based amino and thiol adducts was developed from (+)-neoisopulegol, derived from commercially available (−)-isopulegol. Michael addition of different nucleophiles towards its highly active α,β-unsaturated γ-lactone motif was accomplished, resulting in diverse amino and thiol analogs in [...] Read more.
A library of neoisopulegol-based amino and thiol adducts was developed from (+)-neoisopulegol, derived from commercially available (−)-isopulegol. Michael addition of different nucleophiles towards its highly active α,β-unsaturated γ-lactone motif was accomplished, resulting in diverse amino and thiol analogs in stereoselective reactions. Then, the lactone ring was opened, with NH3 and benzylamine furnishing primary amide and N-benzyl-substituted amide derivatives, respectively. The in vitro antimicrobial effect of prepared compounds was also explored. The results revealed that naphthylmethyl-substituted β-aminolactone, the most promising compound, displayed selective inhibition for the Gram-positive bacteria S. aureus with an MIC (minimum inhibitory concentration) value of 12.5 μM. A docking study was performed to interpret the obtained results. Full article
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