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  • Title: Synthesis and antimicrobial activity of polyhalobenzonitrile quinazolin-4(3H)-one derivatives.
    Author: Shi LP, Jiang KM, Jiang JJ, Jin Y, Tao YH, Li K, Wang XH, Lin J.
    Journal: Bioorg Med Chem Lett; 2013 Nov 01; 23(21):5958-63. PubMed ID: 24044873.
    Abstract:
    A novel series of polyhalobenzonitrile quinazolin-4(3H)-one derivatives were synthesized and characterized by NMR, IR, MS, and HRMS spectra. All of the newly prepared compounds were screened for antimicrobial activities against four strains of bacteria (Gram-positive bacterial: Staphylococcus aureus and Bacillus cereus; Gram-negative bacterial: Escherichia coli and Pseudomonas aeruginosa) and one strain of fungi (Candida albicans). Among the synthesized compounds, 5-(dimethylamino)-8-(2,4,5-trichloro-isophthalonitrile) quinazolin-4(3H)-one (7k) exhibited significant activity towards Gram-positive bacterial, Gram-negative bacterial, and the fungi strains. The MIC (0.8-3.3μg/mL) and MBC (2.6-7.8μg/mL) for this compound were close to those of nofloxacin, chlorothalonil, and fluconazole, making it the most potent antimicrobial agents in the series.
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