Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
Review
. 2022 Apr 25:9:864286.
doi: 10.3389/fmolb.2022.864286. eCollection 2022.

Triazoles and Their Derivatives: Chemistry, Synthesis, and Therapeutic Applications

Affiliations
Review

Triazoles and Their Derivatives: Chemistry, Synthesis, and Therapeutic Applications

Mohammed M Matin et al. Front Mol Biosci. .

Abstract

Among the nitrogen-containing heterocyclic compounds, triazoles emerge with superior pharmacological applications. Structurally, there are two types of five-membered triazoles: 1,2,3-triazole and 1,2,4-triazole. Due to the structural characteristics, both 1,2,3- and 1,2,4-triazoles are able to accommodate a broad range of substituents (electrophiles and nucleophiles) around the core structures and pave the way for the construction of diverse novel bioactive molecules. Both the triazoles and their derivatives have significant biological properties including antimicrobial, antiviral, antitubercular, anticancer, anticonvulsant, analgesic, antioxidant, anti-inflammatory, and antidepressant activities. These are also important in organocatalysis, agrochemicals, and materials science. Thus, they have a broad range of therapeutic applications with ever-widening future scope across scientific disciplines. However, adverse events such as hepatotoxicity and hormonal problems lead to a careful revision of the azole family to obtain higher efficacy with minimum side effects. This review focuses on the structural features, synthesis, and notable therapeutic applications of triazoles and related compounds.

Keywords: SARS-CoV-2; anticancer agents; azide–alkyne cycloaddition; cefatrizine; isomeric triazoles; microwave-assisted green synthesis; pharmacological applications; triazole–thiazole hybrids.

PubMed Disclaimer

Conflict of interest statement

The authors declare that the research was conducted in the absence of any commercial or financial relationships that could be construed as a potential conflict of interest.

Figures

FIGURE 1
FIGURE 1
Medicinal drugs with triazole nucleus.
FIGURE 2
FIGURE 2
Structures of isomeric triazoles.

References

    1. Abdulghani S. M., Al-Rawi M. S., Tomma J. H. (2022). Synthesis of New 1,2,4-triazole Derivatives with Expected Biological Activities. Chem. Methodol. 6 (1), 59–66. 10.22034/chemm.2022.1.6 - DOI
    1. Albert A., Taylor P. J. (1989). The Tautomerism of 1,2,3-triazole in Aqueous Solution. J. Chem. Soc. Perkin Trans. 2 2, 1903–1905. 10.1039/P29890001903 - DOI
    1. Aneja B., Azam M., Alam S., Perwez A., Maguire R., Yadava U., et al. (2018). Natural Product-Based 1,2,3-triazole/sulfonate Analogues as Potential Chemotherapeutic Agents for Bacterial Infections. ACS Omega 3, 6912–6930. 10.1021/acsomega.8b00582 - DOI - PMC - PubMed
    1. Aouad M. R., Khan D. J. O., Said M. A., Al‐Kaff N. S., Rezki N., Ali A. A., et al. (2021). Novel 1,2,3‐Triazole Derivatives as Potential Inhibitors against Covid‐19 Main Protease: Synthesis, Characterization, Molecular Docking and DFT Studies. ChemistrySelect 6, 3468–3486. 10.1002/slct.202100522 - DOI - PMC - PubMed
    1. Avula S. K., Khan M., Halim S. A., Khan A., Al-Riyami S. A., Csuk R., et al. (2021). Synthesis of New 1H-1,2,3-Triazole Analogs in Aqueous Medium via "Click" Chemistry: A Novel Class of Potential Carbonic Anhydrase-II Inhibitors. Front. Chem. 9, 642614. 10.3389/fchem.2021.642614 - DOI - PMC - PubMed