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Synthesis of Cationic Biphen[4, 5]arenes as Biofilm Disruptors.
Du, Xinbei; Ma, Mengke; Zhang, Yahan; Yu, Xiang; Chen, Longming; Zhang, Han; Meng, Zhao; Jia, Xueshun; Chen, Junyi; Meng, Qingbin; Li, Chunju.
Affiliation
  • Du X; Department of Chemistry, Center for Supramolecular Chemistry and Catalysis, Shanghai University, Shanghai, 200444, P. R. China.
  • Ma M; State Key Laboratory of Toxicology and Medical Countermeasures, Beijing Institute of Pharmacology and Toxicology, Beijing, 100850, P. R. China.
  • Zhang Y; State Key Laboratory of Toxicology and Medical Countermeasures, Beijing Institute of Pharmacology and Toxicology, Beijing, 100850, P. R. China.
  • Yu X; State Key Laboratory of Toxicology and Medical Countermeasures, Beijing Institute of Pharmacology and Toxicology, Beijing, 100850, P. R. China.
  • Chen L; Department of Chemistry, Center for Supramolecular Chemistry and Catalysis, Shanghai University, Shanghai, 200444, P. R. China.
  • Zhang H; State Key Laboratory of Toxicology and Medical Countermeasures, Beijing Institute of Pharmacology and Toxicology, Beijing, 100850, P. R. China.
  • Meng Z; State Key Laboratory of Toxicology and Medical Countermeasures, Beijing Institute of Pharmacology and Toxicology, Beijing, 100850, P. R. China.
  • Jia X; State Key Laboratory of Toxicology and Medical Countermeasures, Beijing Institute of Pharmacology and Toxicology, Beijing, 100850, P. R. China.
  • Chen J; State Key Laboratory of Toxicology and Medical Countermeasures, Beijing Institute of Pharmacology and Toxicology, Beijing, 100850, P. R. China.
  • Meng Q; Department of Chemistry, Center for Supramolecular Chemistry and Catalysis, Shanghai University, Shanghai, 200444, P. R. China.
  • Li C; State Key Laboratory of Toxicology and Medical Countermeasures, Beijing Institute of Pharmacology and Toxicology, Beijing, 100850, P. R. China.
Angew Chem Int Ed Engl ; 62(21): e202301857, 2023 05 15.
Article in En | MEDLINE | ID: mdl-36929684
Since bacteria in biofilms are inherently resistant to antibiotics and biofilm-associated infections pose a serious threat to global public health, new therapeutic agents and schemes are urgently needed to meet clinical requirements. Here two quaternary ammonium-functionalized biphen[n]arenes (WBPn, n=4, 5) were designed and synthesized with excellent anti-biofilm potency. Not only could they inhibit the assembly of biofilms, but also eradicate intractable mature biofilms formed by Gram-positive S. aureus and Gram-negative E. coli bacterial strains. Moreover, they could strongly complex a conventional antibiotic, cefazolin sodium (CFZ) with complex stability constants of (7.41±0.29)×104  M-1 for CFZ/WBP4 and (4.98±0.49)×103  M-1 for CFZ/WBP5. Combination of CFZ by WBP4 and WBP5 synergistically enhanced biofilm eradication performance in vitro and statistically improved healing efficacy on E. coli-infected mice models, providing a novel supramolecular strategy for combating biofilm-associated infections.
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Staphylococcus aureus / Escherichia coli Limits: Animals Language: En Journal: Angew Chem Int Ed Engl Year: 2023 Document type: Article Country of publication: Germany

Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Staphylococcus aureus / Escherichia coli Limits: Animals Language: En Journal: Angew Chem Int Ed Engl Year: 2023 Document type: Article Country of publication: Germany