Preparation of 8-hydroxyquinoline derivatives as potential antibiotics against Staphylococcus aureus

  • Bioorg Med Chem Lett. 2014 Jan 1;24(1):367-70. doi: 10.1016/j.bmcl.2013.10.072.
Kim-Hung Lam  1 Roberto Gambari  2 Kenneth Ka-Ho Lee  3 Yi-Xin Chen  4 Stanton Hon-Lung Kok  3 Raymond Siu-Ming Wong  3 Fung-Yi Lau  3 Chor-Hing Cheng  5 Wai-Yeung Wong  6 Zhao-Xiang Bian  7 Albert Sun-Chi Chan  8 Johnny Cheuk-On Tang  9 Chung-Hin Chui  10
Affiliations
  • 1. State Key Laboratory of Chirosciences, Department of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University, Hong Kong, China. Electronic address: [email protected].
  • 2. Centre of Biotechnology, Department of Life Sciences and Biotechnology, The University of Ferrara, Ferrara, Italy.
  • 3. School of Biomedical Sciences and Department of Medicine and Therapeutics, The Chinese University of Hong Kong, Hong Kong, China.
  • 4. Department of Chemistry, Guangzhou University, Guangzhou, People's Republic of China.
  • 5. State Key Laboratory of Chirosciences, Department of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University, Hong Kong, China.
  • 6. Institute of Creativity, Department of Chemistry and Institute of Advanced Materials, Hong Kong Baptist University, Waterloo Road, Kowloon Tong, Hong Kong, China.
  • 7. Clinical Division, School of Chinese Medicine, Hong Kong Baptist University, Waterloo Road, Kowloon Tong, Hong Kong, China.
  • 8. Institute of Creativity, Department of Chemistry and Institute of Advanced Materials, Hong Kong Baptist University, Waterloo Road, Kowloon Tong, Hong Kong, China; Clinical Division, School of Chinese Medicine, Hong Kong Baptist University, Waterloo Road, Kowloon Tong, Hong Kong, China.
  • 9. State Key Laboratory of Chirosciences, Department of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University, Hong Kong, China. Electronic address: [email protected].
  • 10. State Key Laboratory of Chirosciences, Department of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University, Hong Kong, China; School of Biomedical Sciences and Department of Medicine and Therapeutics, The Chinese University of Hong Kong, Hong Kong, China; Clinical Division, School of Chinese Medicine, Hong Kong Baptist University, Waterloo Road, Kowloon Tong, Hong Kong, China. Electronic address: [email protected].
Abstract

This work describes the preparation of quinoline compounds as possible anti-bacterial agents. The synthesized quinoline derivatives show anti-bacterial activity towards Staphylococcus aureus. It is interesting to observe that the synthetic 5,7-dibromo-2-methylquinolin-8-ol (4) shows a similar minimum inhibitory concentration of 6.25μg/mL as compared to that of methicillin (3.125μg/mL) against Staphylococcus aureus.

Keywords
Antibacterial agents; Antibiotics; Quinolines; Staphylococcus aureus.