Click Chemistry-Aided Drug Discovery
A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Medicinal Chemistry".
Deadline for manuscript submissions: 15 February 2026 | Viewed by 19
Special Issue Editor
Interests: click chemistry; macrocycles; drug design; metalloproteases; KTGS; medicinal chemistry; chemical probes; chemical space; new modalities
Special Issues, Collections and Topics in MDPI journals
Special Issue Information
Dear Colleagues,
Click chemistry has had an enormous impact on drug discovery, as it has provided chemists with an arsenal of selective, high-yielding, and modular reactions to rapidly assemble and optimize bioactive molecules. This Special Issue aims to highlight advances in the application of click chemistry at all steps of the drug discovery process—from the design and synthesis of diverse compound libraries to targeted delivery systems and chemical probes for biological evaluation.
Topics of interest will include common click reactions, such as copper catalyzed azide–alkyne cycloadditions (CuAAC), strain-promoted cycloadditions, and bio-orthogonal reactions that facilitate in situ modifications and tracking in living systems.
Contributions to the Special Issue will showcase examples of how click chemistry can improve lead identification and structure–activity relationship (SAR) studies, facilitate the isolation and modification of natural products, and provide new therapeutic modalities (including macrocycles and PROTACs). By presenting original research, reviews, and short communications, this Special Issue is expected to provide a snapshot of how click chemistry is expanding the medicinal chemistry toolbox, presenting new solutions to problems that have challenged drug development for years.
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
- structure–activity relationship
- hit-to-lead
- chemical probes
- bio-orthogonal reactions
- protein-templated reactions
- bioisosteres
- cycloaddition
- 1,2,3-triazole
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