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.


Abstract

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. https://doi.org/10.9734/ajocs/2024/v14i3305

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