Importance and Involvement of Imidazole Structure in Current and Future Therapy

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.

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Journal
Molecules
Published
2026-01-26
DOI
https://doi.org/10.3390/molecules31030423
Primary Topic
Synthesis and biological activity
Type
article
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article

Importance and Involvement of Imidazole Structure in Current and Future Therapy

Ilioara Oniga, Maria Drăgan, Ovidiu Oniga, Oana-Maria Dragostin et al.
Molecules
Synthesis and biological activity
article

Importance and Involvement of Imidazole Structure in Current and Future Therapy

Ilioara Oniga, Maria Drăgan, Ovidiu Oniga, Oana-Maria Dragostin, Elena Lăcrămioara Lisă, C. Ştefan, Alexandra Pavel Burlacu, Mădălina Nicoleta Matei
article en

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.

MoleculesVol. 31(3)
Iuliu Hațieganu University of Medicine and Pharmacy (RO), Grigore T. Popa University of Medicine and Pharmacy (RO), "Dunarea de Jos" University of Galati (RO)
Good health and well-being
Openalex Percentile: Top 77%
Synthesis and biological activity
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Importance and Involvement of Imidazole Structure in Current and Future Therapy — Ilioara Oniga, Maria Drăgan, et al. · Molecules (2026) | TGRS Research Map | TGRS