Innovative Organic Synthesis Approaches in Drug Design and Development
A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Medicinal Chemistry".
Deadline for manuscript submissions: 30 April 2026 | Viewed by 12
Special Issue Editors
Interests: organic synthesis; bio-polymers; green chemistry; pharmacologically active molecules
Interests: synthesis of heterocycles with potential biological activity; Lewis acid catalysis; enantioselective organocatalysis; 1,3-Dipolar cycloadditions in non-conventional solvents; synthesis of new innovative materials
Special Issues, Collections and Topics in MDPI journals
Special Issue Information
Dear Colleagues,
The development of novel therapeutics is increasingly dependent on innovative, efficient and sustainable organic synthesis strategies. While traditional methods are foundational to medicinal chemistry, they often involve lengthy synthetic sequences, limited atom economy and extensive use of toxic reagents or volatile organic solvents. To address these challenges, the field is shifting towards methodologies that combine chemical innovation with the principles of green chemistry. This approach fosters safer, cleaner and more resource-efficient drug discovery pipelines. This Special Issue showcases recent advances in synthetic methodologies that directly impact drug design and development. Topics of interest include transition-metal catalysis, Lewis Acid catalysis, photoredox and electrochemical transformations, organocatalysis, multicomponent reactions, flow chemistry and hybrid molecule approaches, combining different activation modes through various different pharmacophore motifs in a single organic structure. Particular emphasis will be placed on methodologies that expand accessible chemical spaces, enable the late-stage functionalization of bioactive molecules and provide higher levels of efficiency, selectivity and scalability. A central theme will be the adoption of non-traditional solvents and environmentally benign reaction conditions. Using ionic liquids, deep eutectic solvents, supercritical fluids and water as alternative media is one way to reduce the ecological footprint of pharmaceutical synthesis. In addition, the adoption of microwave-assisted solvent-free reactions provide a green approach to synthesizing a new bioactive compound. Combined with advances in automation, miniaturization and computationally guided reaction design, these approaches have the potential to transform drug discovery into an innovative process that is aligned with sustainability goals. Through a collection of original research articles, reviews and perspectives, this Special Issue will provide a comprehensive overview of how novel synthetic strategies are reshaping the design and development of therapeutic agents, offering new opportunities for innovation at the interface between synthetic chemistry and sustainable drug discovery and enhancing the biological activity of novel synthesized drugs.
Dr. Antonio Jiritano
Dr. Vincenzo Algieri
Guest Editors
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
- sustainable organic synthesis
- green chemistry
- drug design and development
- non-traditional solvents
- Lewis acid catalysis
- catalytic methodologies
- photoredox and electrochemical methods
- medicinal chemistry innovation
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