Click Reactions in Medicinal Chemistry II
A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Medicinal Chemistry".
Deadline for manuscript submissions: 25 September 2024 | Viewed by 3649
Special Issue Editor
Interests: click chemistry; macrocycles; drug design; metalloproteases; KTGS; medicinal chemistry; chemical probes; chemical space; new modalities.
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Special Issue Information
Dear Colleagues,
Since the term “click chemistry” was coined by K. B. Sharpless 20 years ago, click reactions have been used for their wide range of assets by medicinal chemists. In recognition of the tremendous impact of click chemistry, the Royal Swedish Academy of Sciences awarded the Nobel Prize in Chemistry 2022 to Dr. Carolyn R. Bertozzi, Dr. Morten Meldal, and Dr. K. Barry Sharpless. These “click chemistry” reactions share many features such as a high yield, modularity, large scope, and stereospecificity, which meet the requirements of drug discovery. Indeed, this field is in constant search of methodologies that allow for 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, which 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, and alkenes), nucleophilic substitutions on three-membered heterocycles (epoxides and aziridines), and addition reactions with carbon–carbon multiple bonds or a 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 that stem from diversity-oriented click synthesis or through in situ protein-templated click chemistry. Click reactions are also useful for lead optimization when considering bioisosterism, pharmacophore, linking, and ADME.
For this Special Issue, 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, and the design and optimization of small molecules or new modalities (macrocycles and 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 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. 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 2900 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
- click chemistry
- drug discovery
- chemical probes
- bioorthogonal reactions
- protein-templated reactions
- bioisosteres
- bioconjugation
- cycloaddition
- 1,2,3-triazole
- chemical space
