Piperazine Derivatives: A Privileged Scaffold in Modern Synthesis and Medicinal Chemistry
Ten A. Koizhaiganova R. Bissenbay D. Tursynova B. Zhaxibayeva Z. Yu V.
January 2026John Wiley and Sons Inc
ChemistryOpen
2026#15Issue 1
Interest in piperazine scaffolds continues to rise due to their broad relevance across anti-infective, anticancer, and neuroactive research. This review examines reports published from 2014 to 2024 and organizes current developments by therapeutic class, structural modification strategy, and computational assessment. Substitution patterns involving aryl, heterocyclic, and hybrid groups show consistent effects on target affinity, selectivity, and pharmacokinetic properties. Several series demonstrate strong activity in early biological evaluation, supported by docking and pharmacodynamic trends that highlight recurring structural motifs. Synthetic approaches, including N-functionalization, reductive routes, cross-coupling, C-H activation, microwave-assisted reactions, and flow-based methods, provide diverse access to optimized derivatives. Combined interpretation of synthetic, biological, and computational results outlines reproducible structure–property relationships that guide piperazine-focused design. Future progress is expected to arise from hybrid scaffold engineering, improved strategies for central nervous system delivery, and the integration of predictive machine-learning methods into lead refinement.
anticancer agents , antimicrobials , antipsychotics , heterocyclic synthesis , piperazine , privileged scaffold , structure–activity relationship
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Laboratory of Synthetic and Natural Medicinal Compounds Chemistry, A.B. Bekturov Institute of Chemical Sciences, Almaty, Kazakhstan
Faculty of Chemistry, Al-Farabi Kazakh National University, Almaty, Kazakhstan
Department of Chemistry, Kazakh National Pedagogical University named after Abai, Almaty, Kazakhstan
Laboratory of Synthetic and Natural Medicinal Compounds Chemistry
Faculty of Chemistry
Department of Chemistry
10 лет помогаем публиковать статьи Международный издатель
Книга Публикация научной статьи Волощук 2026 Book Publication of a scientific article 2026