Synthesis and antimicrobial activity of polyhalobenzonitrile quinazolin-4(3H)-one derivatives |
| |
| Authors: | Li-Ping Shi Kun-Ming Jiang Jun-Jie Jiang Yi Jin Yun-Hai Tao Ke Li Xing-Hong Wang Jun Lin |
| |
| Affiliation: | 1. Key Laboratory of Medicinal Chemistry for Natural Resource (Yunnan University), Ministry Education, School of Chemical Science and Technology, Yunnan University, Kunming 650091, PR China;2. Institute of Microbiology, Yunnan University, Kunming 650091, PR China;3. Yunnan Tumor Research Institute, The Third Affiliated Hospital of Kunming Medical University, Kunming 650118, PR China |
| |
| 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 (0.8–3.3 μg/mL) and MBC (2.6–7.8 μg/mL) for this compound were close to those of nofloxacin, chlorothalonil, and fluconazole, making it the most potent antimicrobial agents in the series. |
| |
| Keywords: | Synthesis Antimicrobial activity Gram-positive bacterial Gram-negative bacterial Fungi strains |
| 本文献已被 ScienceDirect 等数据库收录！ |
|
