Introduction
Privileged scaffolds represent important frameworks that play an important role in drug discovery and medicinal chemistry. Their inherent versatility allows medicinal chemists to rapidly generate bioactive compounds, optimize lead molecules, and explore diverse therapeutic areas with improved efficiency. Over the past two decades, extensive research has demonstrated that privileged scaffolds serve as key structural motifs in the design of new small-molecule therapeutics, spanning oncology, infectious diseases, immunological and inflammatory diseases, neurodegenerative disorders, and other disease areas.
The first thematic issue, Privileged Scaffolds in Drug Discovery and Medicinal Chemistry, provided an insightful overview of several representative privileged scaffolds, including triazoles, oxazoles, and carboxamides, highlighting their chemical diversity, biological activity, structure–activity relationships (SAR), and clinically approved drugs derived from these motifs. In this new thematic issue (Part II), we aim to extend the discussion to both reported and emerging privileged scaffolds, with an emphasis on their unique structural features, synthetic accessibility, pharmacological activity, physicochemical and pharmacokinetic properties, in vivo efficacy, and applications in medicinal chemistry and drug discovery campaigns. This thematic issue seeks to provide researchers with deeper insights and a comprehensive understanding of the critical role of privileged scaffolds in advancing medicinal chemistry and developing new therapeutic reagents.
Keywords
Privileged Scaffolds, Drug Design, Drug Discovery, Medicinal Chemistry, Inhibitors, Heterocycles, Metal Complexes, Therapeutical Agents, Drug-Like Properties, Structure-Activity Relationships
Sub-topics
- Design, synthesis, and biological evaluation of privileged scaffolds.
- Structure-activity relationship (SAR), molecular docking, and QSAR studies of privileged scaffolds.
- Strategies for optimizing synthetic routes to privileged scaffolds.
- Metal complexes as privileged scaffolds in drug design and discovery
- Physicochemical properties and pharmacokinetic properties of privileged scaffolds
- Privileged scaffolds as enzyme inhibitors and epigenetic modulators
- Natural products and natural product–inspired privileged scaffolds
