Special Issue "Click Reactions in Medicinal Chemistry"

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: 30 October 2022.

Special Issue Editor

Dr. Damien Bosc
E-Mail Website
Guest Editor
Inserm—Institut Pasteur de Lille, U1177—Drugs and Molecules for Living Systems, Université de Lille, 59006 Lille, France
Interests: click chemistry; macrocycles; drug design; metalloproteases; KTGS; medicinal chemistry; chemical probes; chemical space; new modalities.

Special Issue Information

Dear Colleagues,

Since the term “click chemistry” was coined by K. B. Sharpless 20 years ago, click reactions have offered their wide range of assets to medicinal chemists. These reactions share many features such as high yield, modularity, large scope, and stereospecificity, which meet the requirements of drug discovery. This field is indeed in constant search of methodologies allowing a fast and easy access to large libraries of compounds. The ability to carry out click reactions in biological media is of great interest to medicinal chemists who wish to perform chemistry with biological macromolecules.

The flagship of click chemistry reactions, copper-catalyzed azide-alkyne cycloaddition (CuAAC), has all of these advantages. Moreover, the resulting 1,4-disubstituted 1,2,3-triazoles exhibit favorable physicochemical properties that are particularly appealing for medicinal chemists. In addition to CuAAC, other click reactions are exploited for drug discovery such as cycloadditions involving various reactants (e.g., mesoionics, isocyanides, alkenes), nucleophilic substitutions on three-membered heterocycles (epoxides, aziridines), and addition reactions to carbon–carbon multiple bonds or sulfur-fluoride exchange (SuFEx).

The applications of click reactions in medicinal chemistry are numerous. Almost all facets of drug discovery are involved. For example, bioorthogonal click reactions are convenient for designing chemical probes for target validation and proteomics. Hits can then be identified by screening large libraries stemming from diversity-oriented click synthesis or by in situ protein-templated click chemistry. Click reactions are also useful for lead optimization with considerations of bioisosterism, pharmacophore, linking, and ADME.

For this Special Issue of Pharmaceuticals, comprehensive reviews, original research articles, and short communications highlighting the potential of click reactions in medicinal chemistry and focusing on, but not limited to, the synthesis of privileged scaffolds, the design and optimization of small molecules, or new modalities (macrocycles, PROTACs) for therapeutic applications and proteomics are welcome.

Dr. Damien Bosc
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 papers will be 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. Pharmaceuticals is an international peer-reviewed open access monthly 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 2000 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.


  • click chemistry
  • drug discovery
  • chemical probes
  • bioorthogonal reactions
  • protein-templated reactions
  • bioisosteres
  • bioconjugation
  • cycloaddition
  • 1,2,3-triazole
  • chemical space

Published Papers

This special issue is now open for submission.
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