1. Design, synthesis and evaluation of oxazolopyridinone derivatives as quorum sensing inhibitors
- Author
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Weijin Chen, Panpan Zhang, Ting Guo, Xiaotong Gu, Bingfang Bai, Shenyan Zhang, Xiaohong Chang, Yingmei Wang, and Shutao Ma
- Subjects
Ciprofloxacin ,Clarithromycin ,Organic Chemistry ,Drug Discovery ,Pseudomonas aeruginosa ,Pyocyanine ,Quorum Sensing ,Molecular Biology ,Biochemistry ,Anti-Bacterial Agents - Abstract
The antibiotic crisis is associated with the appearance of multidrug resistant (MDR) pathogens, which has caused severe bacterial infections and imposed a huge burden on modern society. Therefore, there is an urgent need to develop new antibacterial drugs with novel mechanism of action. Here we designed and synthesized three series of benzoxazolone, oxazolopyridinone and 3-(2-hydroxyphenyl)hydantoin derivatives and evaluated their activity as novel quorum sensing (QS) inhibitors. We found that benzoxazolone and oxazolopyridinone derivatives had promising QS inhibitory activity in the minimum inhibitory concentration, pyocyanin and rhamnolipid inhibition assays. In particular, A10 and B20 at 256 μg/mL not only suppressed pyocyanin production regulated by QS in P. aeruginosa PAO1 by 36.55% and 46.90%, respectively, but also showed the strongest rhamnolipid inhibitory activity with the IC
- Published
- 2022