Synthesis, Antimicrobial Assessment of Chalcones and their Pyrimidine Derivatives

Azibanasamesa D.C. Owaba *

Department of Pharmaceutical and Medicinal Chemistry, Faculty of Pharmacy, Niger Delta University, Wilberforce Island, Bayelsa State, Nigeria.

Ebiere Dode

Department of Pharmaceutical and Medicinal Chemistry, Faculty of Pharmacy, Niger Delta University, Wilberforce Island, Bayelsa State, Nigeria.

Ubong B. Bassey

Department of Pharmaceutical and Medicinal Chemistry, Faculty of Pharmacy, Niger Delta University, Wilberforce Island, Bayelsa State, Nigeria.

*Author to whom correspondence should be addressed.


The aim of the study was to transform chalcones synthesized to their respective pyrimidine derivatives which was successful. The synthesized compounds were subjected to antimicrobial assay against bacteria and fungi organisms screened, however sample ZB had inhibitory effect against bacterial strains. Sample ZB is active against S. aureus and E. coli with an MIC of 5 and 1 mg/mL with a zone of inhibition 11 and 23 mm respectively. When compared to sample B had activity against E. coli with a minimum inhibitory concentration of 0.1 mg/mL and zone of inhibition of 20 mm. Modification of 4-(2-hydroxyphenyl)-6-(2,3,4-trimethoxyphenyl)pyrimidin-2-one to pyrimidin-2-one increases spectrum of activity against gram positive bacterial S. aureus. Sample A inhibits B. subtilis and P. marneffei with an MIC of   10 mg/mL with a zone of inhibition of 14 mm and 20 mm respectively. Transformation of Sample A to 2-aminopyrimidine drastically abolish the antibacterial and antifungal effect. Sample ZA is inactive against bacteria and fungi organisms, when compared to ZB which inhibits S. aureus and E. coli. The spectral analysis revealed that the samples are in line with literature and had a melting point (100-103oC and 115-117oC) for sample ZA and ZB respectively. The starting materials had a melting point (55-57oC and 95-100oC) for Sample A and B respectively.

Keywords: Chalcones, pyrimidine, antimicrobial, spectroscopy, heterocyclic compounds

How to Cite

Owaba, A. D., Dode, E., & Bassey, U. B. (2024). Synthesis, Antimicrobial Assessment of Chalcones and their Pyrimidine Derivatives. Asian Journal of Chemical Sciences, 14(3), 9–14.


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Owaba ADC, Oyeintonbra M, Raji RO, Chalcones as synthon for heterocyclic compounds- A review. International Journal of Current Research. 2020;12(09): 13672-13681. Doi:

Owaba ADC, Kemelayefa OJ, Eboh AS, Synthesis of Benzylideneacetophenone and anti-seizure determination in experimental rodents, International Journal of Chemistry Studies. 2021;5(1):38-43.

Tylińska V, Wiatrak B, Czyżnikowska Ż, Cieśla-NiechwiadowiczA, Gębarowska E, Janicka-Kłos A, Novel pyrimidine derivatives as potential anticancer agents: synthesis, biological evaluation and molecular docking study. International Journal Molecules Science.2021. DOI: 10.3390/ijms22083825

Owaba ADC, Kemelayefa OJ, Miediegha O, Anticonvulsant appraisalof benzylideneacetophenone analogues in Swiss mice. The Nigerian Journal of Pharmacy. 2022;56(2):217-225.

Farooq S, NgainiZ. Chalcone derived pyrazole synthesis via one-pot and two-pot strategies. Current Organic Chemistry. 2020;24:1491-1506. Available:

Rammohan A, Reddy J, Sravya G, Rao C, Zyryanov G. Chalcone synthesis, properties and medicinal applications: A review. Environmental Chemistry Letters. 2020;18:433-458. Available:

Borge V, Patil R. Comparative study on synthesis and biological, pharmaceutical applications of aromatic substituted chalcones. Mini-Reviews in Organic Chemistry;2022. Available:

Leitão E. Chalcones: Retrospective synthetic approaches and mechanistic aspects of a privileged scaffold. Current PharmaceuticalDesign; 2020.Available:

Shetty C, Dikshith L, Dsouza F, Shahana F, Nooha F. Synthesis and evaluation of antibacterial properties of chalcones derived from thiophene-2-carbaldehyde. Journal of Pharmaceutical Research International; 2021. Available:

Rajendran G, Bhanu D, Aruchamy B, Ramani P, Pandurangan N, Bobba K, Oh E, Chung H, Gangadaran P, Ahn B. Chalcone: A promising bioactive scaffold in medicinal chemistry. Pharmaceuticals. 2022;15. Available:

Morsy N, Hassan A. Synthesis, reactions, and applications of chalcones: A review. European Journal of Chemistry; 2022. Available:

Baba H, Usifoh CO, Onanuga A, Antibacterial screening of some synthesized palmitoyl amino acids and their aromatic analogues. British Journal of Pharmaceutical Research. 2014;4(4):513-519.

Kachroo M, Panda R Yadav, Synthesis Y. Biological activities of some new pyrimidine derivatives from chalcones. Der Pharma Chemica. 2014:6(2):352-35.

Sahoo BM, RajeswariM, Jnyanaranjan P, Sahoo B. Green expedient synthesis of pyrimidine derivatives via chalcones and evaluation of their anthelmintic activity, Indian Journal of Pharmaceutical Education and Research. 2017;51(4S).

Kaur N, Dhawan RK, Singh B. Green synthesis of pyrimidine derivatives via chalcones and Their Biological Evaluation International Journal of Research in Engineering and Science. 2021;09(12);59-66.

Sharma YR. Elementary organic spectroscopy: Principles and Chemical Application. S. Chand and Company PVT. Ltd.New York.2015;162.

Kalsi PS. Spectroscopy of organic compounds. 3rd edition. New Age International Publishers, New Delhi, India.2004;183.

Furniss BS, Hannaford, AJ, Smith PWG, Tatchell AR Vogel’s textbook of practical organic chemistry, 5th ednpearsonEducation Limited, Edinburgh Gate Harlow, Essex CM20 2JE England. 1989;1412-1422.