Synthesis of pyrimidinone derivatives and their antimicrobial activity
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Date
2023
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Punjab Agricultural University
Abstract
An efficient protocol has been used for the synthesis of pyrimidinone derivatives via a onepot three-component condensation reaction of aryl aldehydes, malononitrile and barbituric acid in aqueous conditions using tetrabutylammonium hydrogen sulfate. A simple procedure, short reaction time, high yields (78–93 %), broader substrate scope, easy handling of the catalyst and simple work-up, i.e., non-column chromatographic separation of the desired products were attractive features of this process. The structures of synthesized derivatives (4aj) were confirmed by spectral analysis. The in vitro antimicrobial activity of the compounds was determined by the agar well diffusion method against Dickeya sp. (Gram-negative bacteria) and Streptomyces scabiei (Gram-positive bacteria). The synthesized compounds exhibited zone of inhibition at 10.67 ± 0.33, 9.50 ± 0.29 and 10.75 ± 0.14 mm in diameter for (4f), (4g) and (4j) respectively against Dickeya sp., compared to Gentamicin as standard (zone of inhibition at 19.17 ± 0.22 mm). The compounds were found to be potent towards the antioxidant activity. Using H2O2 scavenging assay, the derivatives (4g), (4j), (4i) and (4f) emerged to display promising antioxidant activities with inhibition percentages at 82.01 ± 0.28, 81.57 ± 0.34, 80.97 ± 0.19 and 76.97 ± 0.29 respectively, similar to the ascorbic acid and gallic acid (percent inhibition of 80.46 ± 0.32 and 79.51 ± 0.10, respectively) used as reference standards.
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Baljinder Kaur (2023). Synthesis of pyrimidinone derivatives and their antimicrobial activity (Unpublished M.Sc. thesis). Punjab Agricultural University, Ludhiana, Punjab, India.