Synthesis of Cationic Biphen[4, 5]arenes as Biofilm Disruptors.
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.â
aureus and Gram-negative E.â
coli bacterial strains. Moreover, they could strongly complex a conventional antibiotic, cefazolin sodium (CFZ) with complex stability constants of (7.41±0.29)×104 â
M-1 for CFZ/WBP4 and (4.98±0.49)×103 â
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.â
coli-infected mice models, providing a novel supramolecular strategy for combating biofilm-associated infections.
Key words
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