A systematic review published in BMC Chemistry has compiled six years of research on piperazine derivatives, identifying several compounds with striking activity against bacteria, tuberculosis, cancer cells and Zika virus.
Piperazine, a nitrogen-containing heterocycle, is among the most widely used scaffolds in the development of pharmacologically active molecules. Its adaptable structure has made it a favoured building block for novel bioactive compounds over many years.
Despite this popularity, the authors note a lack of comprehensive information on the current state of piperazine synthesis and medicinal applications. Their review therefore set out to compile research articles published between 2020 and 2025 covering both synthetic methodologies and biological activities.
The papers were gathered from major databases and search engines, and the review covers a broad range of reported derivatives rather than a single study or compound class.
Among the compiled findings, four compounds stood out as antibacterial leads. Compounds 41b, 41d, 42f and 43e each showed a minimum inhibitory concentration of 0.391 micrograms per millilitre against Staphylococcus aureus, a value the review highlights as promising.
Against Mycobacterium tuberculosis, compound 98a achieved an MIC of 0.65 micrograms per millilitre. In cancer research, compound 207f recorded an IC50 of 1.86 plus or minus 0.03 micromolar against the MCF-7 breast cancer cell line, a laboratory measurement rather than a clinical result.
Antiviral activity was also reported: compound 218i showed an EC50 of 0.82 plus or minus 0.33 micromolar against Zika virus. These figures come from in vitro and cell-based assays compiled in the review, not from human trials.
The review is described as an early-access, peer-reviewed accepted article, and its authors are Abdulmenan Shemsu, Abel Abebaw, Ephriem Tadesse and Tsegu Kiros.
The authors suggest the compilation could benefit researchers as a source of up-to-date preliminary information, highlighting synthetic routes and medicinal applications of piperazine derivatives for future work.
As a systematic review, the article summarises existing literature rather than presenting new laboratory experiments, and the highlighted compounds remain candidates for further study rather than approved treatments.
Subject of Research: Synthesis and biological activities of piperazine derivatives, 2020–2025
Article Title: Synthesis and diverse biological activities of piperazine derivatives: a systematic review on their current status (2020–2025)
Article References: Shemsu, A., Abebaw, A., Tadesse, E., & Kiros, T. (2026). Synthesis and diverse biological activities of piperazine derivatives: a systematic review on their current status (2020–2025). BMC Chemistry. https://doi.org/10.1186/s13065-026-01952-5
Image Credits: AI Generated
DOI: 10.1186/s13065-026-01952-5
Keywords: piperazine, systematic review, antibacterial, tuberculosis, breast cancer, Zika virus, medicinal chemistry, heterocycles, MIC, drug discovery, Synthesis, diverse
News Source: Bethany Barker. (October 28, 2026). Piperazine Derivatives Show Potent Antimicrobial and Anticancer Activity in Review. Scienmag.
