# Importance and Involvement of Imidazole Structure in Current and Future Therapy

**Authors:** Alexandra Pavel Burlacu, Maria Drăgan, Ovidiu Oniga, Mădălina Nicoleta Matei, Ilioara Oniga, Elena-Lăcrămioara Lisă, Claudia-Simona Stefan, Oana-Maria Dragostin

PMC · DOI: 10.3390/molecules31030423 · Molecules · 2026-01-26

## TL;DR

This review discusses the importance of imidazole in drug development, highlighting its role in improving pharmacological properties and its potential in cancer and other therapies.

## Contribution

The paper reviews recent advances in imidazole derivatives, emphasizing their medicinal potential and structural modifications for improved therapeutic outcomes.

## Key findings

- Imidazole derivatives show significant anticancer activity by inhibiting tumor cell metabolic pathways.
- Nitroimidazoles target hypoxic tumor tissues, while mercaptopurine derivatives are effective in oncological treatments.
- Structural modifications of imidazole increase selective cytotoxicity against cancer cells.

## Abstract

Imidazole is, from a structural point of view, a heterocycle consisting of three C atoms and two N atoms, belonging to the class of diazoles, having two N atoms at the first and third positions in the aromatic ring. Being a polar and ionizable aromatic compound, it has the role of improving the pharmacological properties of lead molecules, thus being used to optimize their solubility and bioavailability. Imidazole is a constituent of many important biological compounds, like histidine, histamine, and purine compounds, the most widespread heterocyclic compound in nature. In current practice, substituted imidazole derivatives play a major role in antifungal, antibacterial, anti-inflammatory, CNS active compounds, antiprotozoal, as well as anticancer therapy. Thus, imidazole derivatives have demonstrated significant anticancer activities by inhibiting the key metabolic pathways essential for tumor cell growth and survival. Nitroimidazoles, for instance, have been employed as hypoxia-directed therapeutic agents, targeting oxygen-deprived tumor tissues, while mercaptopurine derivatives are well-established in oncological treatments. Structural modifications of the imidazole nucleus have led to the novel compounds exhibiting increased selective cytotoxicity against cancer cells, while sparing normal healthy cells. In accordance with what has been stated, this review highlights recent research on the medicinal and pharmaceutical interest of novel imidazole derivatives, emphasizing their potential in the development of new drugs.

## Linked entities

- **Chemicals:** imidazole (PubChem CID 795), histidine (PubChem CID 773), histamine (PubChem CID 774), purine (PubChem CID 1044), nitroimidazoles (PubChem CID 10701), mercaptopurine (PubChem CID 667490)
- **Diseases:** cancer (MONDO:0004992)

## Full-text entities

- **Diseases:** cancer (MESH:D009369), cytotoxicity (MESH:D064420), hypoxia (MESH:D000860), inflammatory (MESH:D007249)
- **Chemicals:** Imidazole (MESH:C029899), histamine (MESH:D006632), N (MESH:D009584), diazoles (-), Nitroimidazoles (MESH:D009593), mercaptopurine (MESH:D015122), purine (MESH:C030985), C (MESH:D002244), oxygen (MESH:D010100), histidine (MESH:D006639)

## Full text

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## Figures

36 figures with captions in the complete paper: https://tomesphere.com/paper/PMC12899906/full.md

## References

147 references — full list in the complete paper: https://tomesphere.com/paper/PMC12899906/full.md

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Source: https://tomesphere.com/paper/PMC12899906