Definition and research guide
This page combines a MeSH definition, publication statistics and selected research abstracts. It is a starting point for reading the literature, not a medical textbook or a systematic evidence review.
Content available: 4 complete abstracts (727 words), 10 references. Full article text is not stored or reproduced here; follow the PMID, DOI or PMC links to read the original sources and their access terms.
Definition
An anti-nematodal agent effective against the intestinal nematodes ascaris lumbricoides (roundworm) and enterobius vermicularis (pinworm, threadworm). It produces a neuromuscular block leading to flaccid muscle paralysis in susceptible worms, which are then dislodged from the gut and expelled in feces.
Definition: NLM Medical Subject Headings (MeSH) scope note (Public domain (U.S. National Library of Medicine); attribution requested). View the MeSH record.
Also known as: 1,4-Piperazine; 1,4 Piperazine; 1,4-Diazacyclohexane; 1,4 Diazacyclohexane; Pripsen; Piperazine Tartrate (1:1), (R-(R*,R*))-isomer; Piperazine Hydrobromide; Piperazine Hexahydrate.
Where it fits in the MeSH classification
- Broader topics
- Piperazines
Related concepts
- Ascaris Lumbricoides
- Enterobius Vermicularis
Research landscape
PubMed indexes 1,326 records tagged with the MeSH heading “Piperazine” (counts retrieved 2026-10-31). 347 of them (26.2%) were published from 2020 onward, and the busiest period so far is through 1999 with 405 records.
Reviews account for 41 records (3.1%) and meta-analyses for 2. Randomized controlled trials number 5 (0.4%) as a share of all records on the topic. Randomized trials make up only a small share of this literature, so much of what is known comes from laboratory, observational or descriptive work.
Show the data
| Period | Records |
|---|---|
| through 1999 | 405 |
| 2000-2009 | 171 |
| 2010-2019 | 403 |
| 2020 onward | 347 |
Publication-type chart data
| Type | Records | Share |
|---|---|---|
| Reviews | 41 | 3.1% |
| Meta-analyses | 2 | 0.2% |
| Randomized controlled trials | 5 | 0.4% |
Method: PubMed query "Piperazine"[MeSH Terms] with publication-type and date filters, retrieved 2026-10-31.
Reading the evidence in drugs and chemicals
Studies of a chemical or drug can answer very different questions: what it is and how it behaves in cells and animals, how the body handles it, and whether it changes outcomes in people. Laboratory and animal findings often do not carry over to patients, and observational studies of exposures are confounded by who uses a substance and why. Nothing on this page is a recommendation to use, avoid, start or stop any substance or medicine; talk to a qualified clinician or pharmacist about your own situation. Check the dose, the species, the comparison group and whether a patient-relevant outcome was measured.
Evidence from open-access studies
These open-access studies come from PubMed’s best-match results for this heading (papers whose main topic it is), ranked here by citation count, with one recent addition. Each abstract is reproduced in full under its recorded open licence so that you can read the authors’ own words. They illustrate the literature; they are not a systematic summary of it. Citation counts measure attention, not reliability or clinical benefit.
| Study / authors | Year | Source label / design | Europe PMC citations | Licence / source |
|---|---|---|---|---|
| A Novel Piperazine-Based Drug Lead for Cryptosporidiosis from the Medicines for Malaria Venture Open-Access Malaria Box | 2018 | Research article Design not recorded in structured metadata | 61 | cc by PMID 29339392 · DOI · PMC5913971 |
| Design, Synthesis and Anticancer Screening of Novel Benzothiazole-Piperazine-1,2,3-Triazole Hybrids | 2018 | Research article Design not recorded in structured metadata | 29 | cc by PMID 30373247 · DOI · PMC6278665 |
| A new antagonist for CCR4 attenuates allergic lung inflammation in a mouse model of asthma | 2017 | Research article Design not recorded in structured metadata | 27 | cc by PMID 29118379 · DOI · PMC5678437 |
| Piperazine Derivatives: A Privileged Scaffold in Modern Synthesis and Medicinal Chemistry | 2026 | Review article Design not recorded in structured metadata | 6 | cc by PMID 41555571 · DOI · PMC12816771 |
A Novel Piperazine-Based Drug Lead for Cryptosporidiosis from the Medicines for Malaria Venture Open-Access Malaria Box [1]
Abstract reading summary — source excerpts
- Opening excerpt
- Cryptosporidiosis causes life-threatening diarrhea in children under the age of 5 years and prolonged diarrhea in immunodeficient people, especially AIDS patients.
- Closing excerpt
- Collectively, these results identify MMV665917 as a promising lead and establish a new method for characterizing potential anticryptosporidial agents.
- Interpretation limits
- Verbatim excerpts from the authors’ abstract; the closing excerpt may describe a finding, limitation or recommendation. Design, population, effect size and uncertainty have not been independently extracted or appraised. Read the complete abstract and linked paper before interpreting the findings.
Read complete abstract (268 words)
Cryptosporidiosis causes life-threatening diarrhea in children under the age of 5 years and prolonged diarrhea in immunodeficient people, especially AIDS patients. The standard of care, nitazoxanide, is modestly effective in children and ineffective in immunocompromised individuals. In addition to the need for new drugs, better knowledge of drug properties that drive in vivo efficacy is needed to facilitate drug development. We report the identification of a piperazine-based lead compound for Cryptosporidium drug development, MMV665917, and a new pharmacodynamic method used for its characterization. The identification of MMV665917 from the Medicines for Malaria Venture Malaria Box was followed by dose-response studies, in vitro toxicity studies, and structure-activity relationship studies using commercial analogues. The potency of this compound against Cryptosporidium parvum Iowa and field isolates was comparable to that against Cryptosporidium hominis Furthermore, unlike nitazoxanide, clofazimine, and paromomycin, MMV665917 appeared to be curative in a NOD SCID gamma mouse model of chronic cryptosporidiosis. MMV665917 was also efficacious in a gamma interferon knockout mouse model of acute cryptosporidiosis. To determine if efficacy in this mouse model of chronic infection might relate to whether compounds are parasiticidal or parasitistatic for C. parvum, we developed a novel in vitro parasite persistence assay. This assay suggested that MMV665917 was parasiticidal, unlike nitazoxanide, clofazimine, and paromomycin. The assay also enabled determination of the concentration of the compound required to maximize the rate of parasite elimination. This time-kill assay can be used to prioritize early-stage Cryptosporidium drug leads and may aid in planning in vivo efficacy experiments. Collectively, these results identify MMV665917 as a promising lead and establish a new method for characterizing potential anticryptosporidial agents.
Abstract reproduced from the open-access article under the recorded cc by licence; © the authors. PMID 29339392 · DOI · PMC5913971
Design, Synthesis and Anticancer Screening of Novel Benzothiazole-Piperazine-1,2,3-Triazole Hybrids [2]
Abstract reading summary — source excerpts
- Opening excerpt
- A library of novel regioselective 1,4-di and 1,4,5-trisubstituted-1,2,3-triazole based benzothiazole-piperazine conjugates were designed and synthesized using the click synthesis approach in the presence and absence of the Cu(I) catalyst.
- Closing excerpt
- Further, we have established a structure activity relationship with respect to the in silico analysis of ADME (adsorption, distribution, metabolism and excretion) analysis and found good agreement with in vitro activity.
- Interpretation limits
- Verbatim excerpts from the authors’ abstract; the closing excerpt may describe a finding, limitation or recommendation. Design, population, effect size and uncertainty have not been independently extracted or appraised. Read the complete abstract and linked paper before interpreting the findings.
Read complete abstract (120 words)
A library of novel regioselective 1,4-di and 1,4,5-trisubstituted-1,2,3-triazole based benzothiazole-piperazine conjugates were designed and synthesized using the click synthesis approach in the presence and absence of the Cu(I) catalyst. Some of these 1,2,3-triazole hybrids possess in their structures different heterocyclic scaffold including 1,2,4-triazole, benzothiazole, isatin and/or benzimidazole. The newly designed 1,2,3-triazole hybrids were assessed for their antiproliferative inhibition potency against four selected human cancer cell lines (MCF7, T47D, HCT116 and Caco2). The majority of the synthesized compounds demonstrated moderate to potent activity against all the cancer cell lines examined. Further, we have established a structure activity relationship with respect to the in silico analysis of ADME (adsorption, distribution, metabolism and excretion) analysis and found good agreement with in vitro activity.
Abstract reproduced from the open-access article under the recorded cc by licence; © the authors. PMID 30373247 · DOI · PMC6278665
A new antagonist for CCR4 attenuates allergic lung inflammation in a mouse model of asthma [3]
Abstract reading summary — source excerpts
- Opening excerpt
- CCR4 is highly expressed on Th2 cells.
- Closing excerpt
- Our study demonstrated that CCR4 blockaded by compound 8a effectively attenuated airway hyperresponsiveness, airway eosinophilia and Th2 cytokines.
- Interpretation limits
- Verbatim excerpts from the authors’ abstract; the closing excerpt may describe a finding, limitation or recommendation. Design, population, effect size and uncertainty have not been independently extracted or appraised. Read the complete abstract and linked paper before interpreting the findings.
Read complete abstract (198 words)
CCR4 is highly expressed on Th2 cells. CCR4 ligands include CCL22 and CCL17. Chemokine-like factor 1 can also mediate chemotaxis via CCR4. We designed and synthetized novel CCR4 antagonists, which were piperazinyl pyridine derivatives, for disrupting the interaction between three ligands and CCR4. We also determined whether these novel CCR4 antagonists could alleviate allergic asthma in a mouse. For identifying the potent compounds in vitro, we used chemotaxis inhibition and competition binding assays induced by CCL22, CCL17 and one of CKLF1's C-terminal peptides, C27. We found compound 8a which showed excellent potency in blocking the interaction of CCR4 and its three ligands. For studying the specificity of compounds, we chose chemotaxis inhibition assays with different receptors and ligands. We found compound 8a had excellent receptor specificity and exerted few influence on the interaction of other receptors and their ligands. In the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay, compound 8a had no obvious cytotoxicity till the higher concentration (16 μM). For determining the potency of compounds in blocking the interaction of CCR4 in vivo, we used the ovalbumin induced allergic asthma model in mice. Our study demonstrated that CCR4 blockaded by compound 8a effectively attenuated airway hyperresponsiveness, airway eosinophilia and Th2 cytokines.
Abstract reproduced from the open-access article under the recorded cc by licence; © the authors. PMID 29118379 · DOI · PMC5678437
Piperazine Derivatives: A Privileged Scaffold in Modern Synthesis and Medicinal Chemistry [4]
Abstract reading summary — source excerpts
- Opening excerpt
- Interest in piperazine scaffolds continues to rise due to their broad relevance across anti-infective, anticancer, and neuroactive research.
- Closing excerpt
- 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.
- Interpretation limits
- Verbatim excerpts from the authors’ abstract; the closing excerpt may describe a finding, limitation or recommendation. Design, population, effect size and uncertainty have not been independently extracted or appraised. Read the complete abstract and linked paper before interpreting the findings.
Read complete abstract (141 words)
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, CH 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.
Abstract reproduced from the open-access article under the recorded cc by licence; © the authors. PMID 41555571 · DOI · PMC12816771
Key reviews and meta-analyses
The most cited review-type papers among PubMed’s best-match results for this heading, listed with bibliographic details only. Follow the links for the full text and access terms.
- Research article Piperazine, a Key Substructure for Antidepressants: Its Role in Developments and Structure-Activity Relationships [5]
- Research article An appraisal of anti-mycobacterial activity with structure-activity relationship of piperazine and its analogues: A review [6]
- Research article Piperazine: A Promising Scaffold with Analgesic and Anti-inflammatory Potential [7]
- Research article Synthetic Approaches to Piperazine-Containing Drugs Approved by FDA in the Period of 2011-2023 [8]
- Research article The Recent Development of Piperazine and Piperidine Derivatives as Antipsychotic Agents [9]
- Research article Therapeutic Efficacy of Piperazine Ferulate Combined With Irbesartan in Diabetic Nephropathy: A Systematic Review and Meta-analysis [10]
References
- Jumani RS, Bessoff K, Love MS, Miller P, Stebbins EE, Teixeira JE, et al.. A Novel Piperazine-Based Drug Lead for Cryptosporidiosis from the Medicines for Malaria Venture Open-Access Malaria Box. . 2018. PMID 29339392 · DOI · PMC5913971
- Aouad MR, Soliman MA, Alharbi MO, Bardaweel SK, Sahu PK, Ali AA, et al.. Design, Synthesis and Anticancer Screening of Novel Benzothiazole-Piperazine-1,2,3-Triazole Hybrids. . 2018. PMID 30373247 · DOI · PMC6278665
- Zhang Y, Wu Y, Qi H, Xiao J, Gong H, Zhang Y, et al.. A new antagonist for CCR4 attenuates allergic lung inflammation in a mouse model of asthma. . 2017. PMID 29118379 · DOI · PMC5678437
- Ten A, Koizhaiganova R, Bissenbay D, Tursynova B, Zhaxibayeva Z, Yu V. Piperazine Derivatives: A Privileged Scaffold in Modern Synthesis and Medicinal Chemistry. . 2026. PMID 41555571 · DOI · PMC12816771
- Kumar RR, Sahu B, Pathania S, Singh PK, Akhtar MJ, Kumar B. Piperazine, a Key Substructure for Antidepressants: Its Role in Developments and Structure-Activity Relationships. ChemMedChem. 2021. PMID 33751807 · DOI
- Girase PS, Dhawan S, Kumar V, Shinde SR, Palkar MB, Karpoormath R. An appraisal of anti-mycobacterial activity with structure-activity relationship of piperazine and its analogues: A review. Eur J Med Chem. 2021. PMID 33190957 · DOI
- Jain A, Chaudhary J, Khaira H, Chopra B, Dhingra A. Piperazine: A Promising Scaffold with Analgesic and Anti-inflammatory Potential. Drug Res (Stuttg). 2021. PMID 33336346 · DOI
- Romanelli MN, Braconi L, Gabellini A, Manetti D, Marotta G, Teodori E. Synthetic Approaches to Piperazine-Containing Drugs Approved by FDA in the Period of 2011-2023. Molecules. 2023. PMID 38202651 · DOI · PMC10780301
- Rathore A, Asati V, Kashaw SK, Agarwal S, Parwani D, Bhattacharya S, et al.. The Recent Development of Piperazine and Piperidine Derivatives as Antipsychotic Agents. Mini Rev Med Chem. 2021. PMID 32912125 · DOI
- Li D, Li B, Peng LX, Liu R, Zeng N. Therapeutic Efficacy of Piperazine Ferulate Combined With Irbesartan in Diabetic Nephropathy: A Systematic Review and Meta-analysis. Clin Ther. 2020. PMID 33158581 · DOI
About this article
- Sources
- NLM Medical Subject Headings (definition, synonyms); NCBI PubMed (counts, identifiers); Europe PMC (open-access abstracts and citation counts).
- Verification
- Every reference was resolved against PubMed on 2026-10-31; title, year and DOI matched.
- Review state
- automated source verified; no human expert review has been recorded yet.
- Version
- 1, last updated 2026-10-31.
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Evidence strength
EvidenceHelix's computed view of the study designs behind this topic: how common meta-analyses, randomized trials and reviews are, how recent the literature is, and a plain-language reading. It describes the design mix of the literature. It is not a quality appraisal of any study, and it is not medical advice.