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 Dec;100(6):818-842.
doi: 10.1111/cbdd.14001. Epub 2021 Dec 27.

Pyrimidine: An elite heterocyclic leitmotif in drug discovery-synthesis and biological activity

Sahaya Nadar  1 , Tabassum Khan  2
Affiliations
Review

Pyrimidine: An elite heterocyclic leitmotif in drug discovery-synthesis and biological activity

Sahaya Nadar et al. Chem Biol Drug Des. 2022 Dec.

Abstract

Heterocyclic compounds bearing the pyrimidine core are of tremendous interest as they constitute an important class of natural and synthetic compounds exhibiting diverse useful biological activities that hold attractive potential for clinical translation as therapeutic agents in alleviation of a myriad of diseases. Heterocycles possessing a pyrimidine scaffold have piqued tremendous interest of organic and medicinal chemists owing to their privileged bioactivities. Drugs having the pyrimidine motif have manifested to exhibit gratifying biological activity like anticancer, antiviral, anti-inflammatory, antibacterial, and antihypertensive activities. This heterocycle, being a significant endogenous component of the body, the pyrimidine derivatives can easily interact with enzymes, genetic materials, and bio components within the cell. The landscape of FDA approved drugs, presently marketed incorporating the pyrimidine scaffold continues to evolve in number and diversity. There is a tremendous surge in discovery of new targets across many diseases especially those involving emerging resistance to clinically used battery of drugs. Pyrimidine scaffolds will continue to be explored expanding their chemical space portfolio in an effort to find novel drugs impacting these targets. This review aims to provide an elaborate recapitulation of the recent trends adopted to synthesize propitious pyrimidine incorporated hits and also focuses on the clinical significance reported for functionalized pyrimidine analogues that would quintessentially aid medicinal chemists for new research explorations in this arena.

Keywords: anti-inflammatory; antibacterial; anticancer; antiviral; pyrimidine; synthesis.

PubMed Disclaimer

References

REFERENCES

    1. Abd El-Hamid, S., Sadeek, S., Zordok, W., & El-Shwiniy, W. (2019). Synthesis, spectroscopic studies, DFT calculations, cytotoxicity and antimicrobial activity of some metal complexes with ofloxacin and 2,2′-bipyridine. Journal of Molecular Structure, 1176, 422-433. https://doi.org/10.1016/j.molstruc.2018.08.082
    1. Abdellatif, K. R. A., & Bakr, R. B. (2018). New advances in synthesis and clinical aspects of pyrazolo[3,4-d]pyrimidine scaffolds. Bioorganic Chemistry, 78, 341-357. https://doi.org/10.1016/j.bioorg.2018.03.032
    1. Abou-Elkhair, R. A. I., Wasfy, A. A., Mao, S., Du, J., Eladl, S., Metwally, K., Hassan, A. E. A., & Sheng, J. (2020). 2-Hydroxyimino-6-aza-pyrimidine nucleosides: synthesis, DFT calculations, and antiviral evaluations. New Journal of Chemistry, 44(45), 19650-19662. http://doi.org/10.1039/d0nj04154h
    1. Acosta, P., Insuasty, B., Ortiz, A., Abonia, R., Sortino, M., Zacchino, S. A., & Quiroga, J. (2016). Solvent-free microwave-assisted synthesis of novel pyrazolo[4′,3′:5,6]pyrido[2,3-d]pyrimidines with potential antifungal activity. Arabian Journal of Chemistry, 9(3), 481-492. https://doi.org/10.1016/j.arabjc.2015.03.002
    1. Addepalli, Y., Yang, X., Zhou, M., Reddy, D. P., Zhang, S.-L., Wang, Z., & He, Y. (2018). Synthesis and anticancer activity evaluation of novel azacalix[2]arene [2]pyrimidines. European Journal of Medicinal Chemistry, 151, 214-225. https://doi.org/10.1016/j.ejmech.2018.02.079

MeSH terms

LinkOut - more resources