Synthesis, Characterization, And Evaluation Of Novel Heterofused Pyrimidine Derivatives As Potential Therapeutic Agents

  • Mrs. Daizy Chouhan
  • Dr. Neelesh Maheshwari
Keywords: Drug discovery, pharmacological evaluation, broad-spectrum efficiency, structural characterization, derivatives containing sulfur, cytotoxicity tests, derivatives of heterofurused pyrimidines, antibacterial and anticancer activities

Abstract

Due to their broad range of biological activities, heterofursed pyrimidine derivatives have been receiving a lot of attention, especially in the context of antimicrobial and anticancer treatments. The goal of this work was to investigate the pharmacological potential of newly discovered heterofused pyrimidine derivatives by synthesizing them using conventional methods. a combination of IR, NMR, and mass spectrometry to evaluate the synthesized compounds structurally, it emerged whether the target derivatives were effectively synthesized. By using human cancer cell lines in vitro cytotoxicity assessments have been used to evaluate their anticancer potential.  The results demonstrated strong activity with IC₅₀ values equivalent to those of conventional chemotherapeutic drugs.  Additionally, antimicrobial activity was evaluated against a panel of fungal and bacterial strains; derivatives containing sulfur were found to have particularly promising broad-spectrum efficacy. These results imply that the produced heterofused pyrimidine derivatives may be useful as starting points for the synthesis of novel antibiotics and anticancer drugs. Future efforts in drug discovery should focus on further optimizing their chemical structures and researching their mechanisms of action.

Author Biographies

Mrs. Daizy Chouhan

Sangam University, Bhilwara, Rajasthan

Dr. Neelesh Maheshwari

Sangam University, Bhilwara, Rajasthan

References

1. Johnson, C. R., & Kirsch, S. L. (2007). Pyrimidine chemistry: A review of synthesis and biological applications. Journal of Medicinal Chemistry, 50(2), 285-297.
2. Kumar, S., Pandey, A., & Singh, R. (2015). Heterocyclic pyrimidine derivatives: Synthesis and medicinal applications. European Journal of Medicinal Chemistry, 97, 30-50.
3. Zhao, Y., Zhang, W., & Liu, B. (2016). Pyrimidine-based anticancer agents: Synthesis, structure-activity relationships, and biological evaluation. Bioorganic & Medicinal Chemistry Letters, 26(7), 1845-1852.
4. Patel, J. R., & Jain, R. K. (2012). Antimicrobial properties of fused pyrimidine derivatives: A comprehensive review. Journal of Antimicrobial Chemotherapy, 67(11), 2773-2784.
5. Al-Saadi, M. S., & Sharaf, A. M. (2017). Synthesis and biological activities of fused pyrimidines. Chemical Reviews, 117(9), 4781-4851.
6. Smith, K. M., & Hager, H. W. (2019). Recent advances in pyrimidine synthesis: Novel approaches and strategies. Current Organic Chemistry, 23(15), 1687-1701.
7. Lopez, J. S., & Bates, D. L. (2020). Novel heterofused pyrimidine derivatives as potential antimicrobial and anticancer agents. Medicinal Chemistry Research, 29(11), 1924-1937.
8. Zhu, X., et al. (2017). Structural modifications in the pyrimidine scaffold: Enhancing anticancer and antimicrobial activity. Journal of Medicinal Chemistry, 60(5), 2023–2035.
9. Roy, D., et al. (2018). Green synthesis of heterofused pyrimidine derivatives using solvent-free and microwave-assisted methods. Organic Chemistry Frontiers, 5(7), 1041–1052.
10. Wang, Y., et al. (2018). Pyrimidine derivatives with triazole and oxazole rings: Enhanced antibacterial and anticancer activities. European Journal of Pharmaceutical Sciences, 119, 59–71.
11. Balbi, A., et al. (2019). Antibacterial and antifungal properties of fused pyrimidine derivatives containing heterocyclic moieties. ChemMedChem, 14(8), 813–826.
12. Kumar, R., et al. (2019). Antibacterial activity of nitrogen-containing fused pyrimidines: Mechanistic insights and structure-activity relationship. Antimicrobial Agents and Chemotherapy, 63(4), e02317-18.
13. Gupta, A., et al. (2020). Preclinical studies of pyrimidine-based compounds: Potent candidates for cancer and infectious diseases. Journal of Clinical Oncology, 38(15_suppl), e15056.
14. Patel, N., et al. (2021). Selective inhibition of colorectal cancer cells by mitochondrial-mediated apoptosis: A study of heterofused pyrimidine derivatives. Oncology Reports, 46(6), 322–332.
15. Singh, P., et al. (2022). Antimicrobial resistance: Potential of pyrimidine compounds fused with nitrogen and sulfur heteroatoms. Journal of Antibiotics, 75(3), 210–222.
16. Zhang, Y., et al. (2023). Antiviral activity of pyrimidine derivatives targeting SARS-CoV-2 viral proteases. Virology Journal, 20(1), 115.
Published
2024-10-26
How to Cite
Mrs. Daizy Chouhan, & Dr. Neelesh Maheshwari. (2024). Synthesis, Characterization, And Evaluation Of Novel Heterofused Pyrimidine Derivatives As Potential Therapeutic Agents. Revista Electronica De Veterinaria, 25(1), 2526 - 2535. https://doi.org/10.69980/redvet.v25i1.1286
Section
Articles