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

Kim-Hung Lam; Roberto Gambari; Kenneth Ka-Ho Lee; Yi-Xin Chen; Stanton Hon-Lung Kok; Raymond Siu-Ming Wong; Fung-Yi Lau; Chor-Hing Cheng; Wai-Yeung Wong; Zhao-Xiang Bian; Albert Sun-Chi Chan; Johnny Cheuk-On Tang; Chung-Hin Chui

doi:10.1016/j.bmcl.2013.10.072

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. Epub 2013 Nov 8.

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].

PMID: 24269165
DOI: 10.1016/j.bmcl.2013.10.072

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Anti-Bacterial Agents / chemical synthesis
Anti-Bacterial Agents / chemistry
Anti-Bacterial Agents / pharmacology*
Cell Death / drug effects
Cell Line
Dose-Response Relationship, Drug
Humans
Microbial Sensitivity Tests
Molecular Structure
Oxyquinoline / chemical synthesis
Oxyquinoline / chemistry
Oxyquinoline / pharmacology*
Staphylococcus aureus / drug effects*
Structure-Activity Relationship

Substances

Anti-Bacterial Agents
Oxyquinoline