Amide Moieties Modulate the Antimicrobial Activities of Conjugated Oligoelectrolytes against Gram-negative Bacteria.
ChemistryOpen
; 11(2): e202100260, 2022 02.
Article
in English
| MEDLINE | ID: covidwho-1704277
ABSTRACT
Cationic conjugated oligoelectrolytes (COEs) are a class of compounds that can be tailored to achieve relevant inâ
vitro antimicrobial properties with relatively low cytotoxicity against mammalian cells. Three distyrylbenzene-based COEs were designed containing amide functional groups on the side chains. Their properties were compared to two representative COEs with only quaternary ammonium groups. The optimal compound, COE2-3C-C3-Apropyl, has an antimicrobial efficacy against Escherichia coli with an MIC=2â
µg mL-1 , even in the presence of human serum albumin low cytotoxicity (IC50 =740â
µg mL-1 ) and minimal hemolytic activity. Moreover, we find that amide groups increase interactions between COEs and a bacterial lipid mimic based on calcein leakage assay and allow COEs to readily permeabilize the cytoplasmic membrane of E. coli. These findings suggest that hydrogen bond forming moieties can be further applied in the molecular design of antimicrobial COEs to further improve their selectivity towards bacteria.
Keywords
Full text:
Available
Collection:
International databases
Database:
MEDLINE
Main subject:
Escherichia coli
/
Anti-Infective Agents
Type of study:
Experimental Studies
/
Randomized controlled trials
Limits:
Animals
/
Humans
Language:
English
Journal:
ChemistryOpen
Year:
2022
Document Type:
Article
Affiliation country:
Open.202100260
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