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Synthesis and Bioactivity of Guanidinium‐Functionalized Pillar[5]arene as a Biofilm Disruptor
Author(s) -
Guo Shuwen,
Huang Qiaoxian,
Chen Yuan,
Wei Jianwen,
Zheng Jun,
Wang Leyong,
Wang Yitao,
Wang Ruibing
Publication year - 2021
Publication title -
angewandte chemie
Language(s) - English
Resource type - Journals
eISSN - 1521-3757
pISSN - 0044-8249
DOI - 10.1002/ange.202013975
Subject(s) - biofilm , chemistry , pillar , bacteria , combinatorial chemistry , microbiology and biotechnology , antibiotics , biochemistry , biology , genetics , structural engineering , engineering
Due to the inherent resistance of bacterial biofilms to antibiotics and their serious threat to global public health, novel therapeutic agents and strategies to tackle biofilms are urgently needed. To this end, we designed and synthesized a novel guanidinium‐functionalized pillar[5]arene (GP5) that exhibited high antibacterial potency against Gram‐negative E. coli (BH101) and Gram‐positive S. aureus (ATCC25904) strains. More importantly, GP5 effectively disrupted preformed E. coli biofilms by efficient penetration through biofilm barriers and subsequent destruction of biofilm‐enclosed bacteria. Furthermore, host–guest complexation between GP5 and cefazolin sodium, a conventional antibiotic that otherwise shows negligible activity against biofilms, exhibited much enhanced, synergistic disruption activity against E . coli biofilms, thus providing a novel supramolecular platform to effectively disrupt biofilms.