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Novel 2, 8-bit derivatives of quinolines attenuate Pseudomonas aeruginosa virulence and biofilm formation.
Qiu, Man-Na; Wang, Fang; Chen, Si-Yu; Wang, Peng-Cheng; Fu, Yu-Hang; Liu, Yuan-Yuan; Wang, Xuan; Wang, Fan-Bei; Wang, Chao; Yang, Hong-Wen; Wu, Yang; Zhu, Shi-Ying; Zhou, Hai-Bo; Chen, Wei-Min; Lin, Jing; Zheng, Jun-Xia; Sun, Ping-Hua.
Affiliation
  • Qiu MN; Guangdong Engineering Research Center of Chinese Medicine & Disease Susceptibility, College of Pharmacy, Jinan University, Guangzhou 510632, PR China.
  • Wang F; Pharmacy Department, Qingdao Stomatological Hospital, Qingdao 266000, PR China.
  • Chen SY; Guangdong Engineering Research Center of Chinese Medicine & Disease Susceptibility, College of Pharmacy, Jinan University, Guangzhou 510632, PR China.
  • Wang PC; Guangdong Engineering Research Center of Chinese Medicine & Disease Susceptibility, College of Pharmacy, Jinan University, Guangzhou 510632, PR China.
  • Fu YH; Guangdong Engineering Research Center of Chinese Medicine & Disease Susceptibility, College of Pharmacy, Jinan University, Guangzhou 510632, PR China.
  • Liu YY; Guangdong Engineering Research Center of Chinese Medicine & Disease Susceptibility, College of Pharmacy, Jinan University, Guangzhou 510632, PR China.
  • Wang X; Guangdong Engineering Research Center of Chinese Medicine & Disease Susceptibility, College of Pharmacy, Jinan University, Guangzhou 510632, PR China.
  • Wang FB; Guangdong Engineering Research Center of Chinese Medicine & Disease Susceptibility, College of Pharmacy, Jinan University, Guangzhou 510632, PR China.
  • Wang C; Department of Chemistry, Yale University, New Haven, CT 06520, United States.
  • Yang HW; Pharmacy Department, Qingdao Stomatological Hospital, Qingdao 266000, PR China.
  • Wu Y; Guangdong Engineering Research Center of Chinese Medicine & Disease Susceptibility, College of Pharmacy, Jinan University, Guangzhou 510632, PR China.
  • Zhu SY; Guangdong Engineering Research Center of Chinese Medicine & Disease Susceptibility, College of Pharmacy, Jinan University, Guangzhou 510632, PR China.
  • Zhou HB; Guangdong Engineering Research Center of Chinese Medicine & Disease Susceptibility, College of Pharmacy, Jinan University, Guangzhou 510632, PR China.
  • Chen WM; Guangdong Engineering Research Center of Chinese Medicine & Disease Susceptibility, College of Pharmacy, Jinan University, Guangzhou 510632, PR China.
  • Lin J; Guangdong Engineering Research Center of Chinese Medicine & Disease Susceptibility, College of Pharmacy, Jinan University, Guangzhou 510632, PR China.
  • Zheng JX; School of Chemical Engineering and Light Industry, Guangdong University of Technology, Guangzhou 510006, PR China. Electronic address: junxiazheng@163.com.
  • Sun PH; Guangdong Engineering Research Center of Chinese Medicine & Disease Susceptibility, College of Pharmacy, Jinan University, Guangzhou 510632, PR China. Electronic address: pinghuasunny@163.com.
Bioorg Med Chem Lett ; 29(5): 749-754, 2019 03 01.
Article in En | MEDLINE | ID: mdl-30630718
ABSTRACT
Signal molecules are stimulators of multiple quroum-sensing virulence and biofilm formation. Small molecule analogues have been suspected as a potent inhibitor in therapeutic strategy. Herein, we synthesized a series of small molecule compounds from the 2, 8-bit derivatives of quinoline by Suzuki coupling reaction. We found that these compounds have the biofilm inhibitory effect in normal condition instead of phosphate limitation state. Furthermore, lacZ reporter strain assay and rhamnolipids as well as pyocyanin experiments showed that these compounds did not affect las and pqs system but reduced the expression of rhl. All these results suggest that quinoline derivatives can be treated as potent inhibitors against biofilm and reduce virulence through the rhl system. This research will be useful in designing new quorum sensing inhibitors to attenuate the infection of bacteria.
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Pseudomonas aeruginosa / Quinolines / Virulence / Biofilms / Anti-Bacterial Agents Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2019 Document type: Article

Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Pseudomonas aeruginosa / Quinolines / Virulence / Biofilms / Anti-Bacterial Agents Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2019 Document type: Article