期刊
FUTURE MEDICINAL CHEMISTRY
卷 8, 期 16, 页码 1927-1940出版社
FUTURE SCI LTD
DOI: 10.4155/fmc-2016-0002
关键词
antibacterial; antifungal; DNA cleavage; DNA intercalation; imidazole; quinazolinone; triazole
资金
- National Natural Science Foundation of China [21372186, 21672173]
- Research Fund for International Young Scientists from International (Regional) Cooperation and Exchange Program NSFC [81450110094]
- Chongqing Special Foundation for Postdoctoral Research Proposal [Xm2015031]
Aim: Due to bacterial drug resistance, a new series of quinazolinone azolyl ethanols were synthesized and evaluated. Results: In vitro antibacterial assay showed that triazolyl ethanol quinazolinone 3a was the most active compound, especially against MRSA with minimal inhibitory concentration value of 8 mu g/ml, which was superior to chloromycin and comparable to norfloxacin. Molecular docking study displayed that compound 3a could interact with MRSA DNA by the formation of hydrogen bonds. Further interactions of quinazolinone 3a with MRSA DNA suggested that it could intercalate into MRSA DNA to form 3a-DNA complex. DNA cleavage properties of 3a-Cu2+ and 3a-Zn2+ complexes were confirmed by agarose gel electrophoresis experiments. Conclusion: Compound 3a should be a potential lead antibacterial molecule with dual action modes.
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