Citation: Yun Xu Yang, Hui Yuan Guo. Synthesis of 6,8-dichloroquinolones utilizing new method and evaluation of their antibacterial activities[J]. Chinese Chemical Letters, ;2007, 18(12): 1479-1482. doi: 10.1016/j.cclet.2007.10.012 shu

Synthesis of 6,8-dichloroquinolones utilizing new method and evaluation of their antibacterial activities

Yun Xu Yang ^a, ,
Hui Yuan Guo ^b

a Department of Chemistry, University of Science and Technology, Beijing 100083, China;
b Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences, Peking Union Medical College, Beijing 100050, China

Received Date: 2 July 2007

Fund Project: The author thanks for the support from the National Research Center for Analysis of Drugs and Metabolites, CAMS PUMC with the ¹H NMR, MS.

Several 6, 8-dichloroquinolone analogues were synthesized from the key intermediate compound of 2, 3, 4, 5-tetrachlorobenzene carbonyl chloride, which was obtained from the starting material of tetrachlorophthalic anhydride. Their in vitro antibacterial activities were evaluated. As a result of this study, compounds 21c and 21d were twofold more potent than ciprofloxacin (CPFX) and norfloxacin (NFLX) against Staphylococcus aureus-9, and with the same potent as CPFX and NFLX while against Escherichia coli-2, but were less potent than references in against Pseudomonas aeruginosa-17.
- Quinolones,
- Synthesis,
- Antibacterial,
- 6,8-Dichloroquinolone
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