Further Investigations into Rigidity-Activity Relationships in BisQAC Amphiphilic Antiseptics.
CHEMMEDCHEM(2020)
Abstract
Thirty-six biscationic quaternary ammonium compounds were efficiently synthesized in one step to examine the effect of molecular geometry of two-carbon linkers on antimicrobial activity. The synthesized compounds showed strong antimicrobial activity against a panel of both Gram-positive and Gram-negative bacteria, including methicillin-resistant Staphylococcus aureus (MRSA). While the linker geometry showed only a modest correlation with antimicrobial activity, several of the synthesized bisQACs are promising potential antiseptics due to good antimicrobial activity (MIC <= 2 mu M) and their higher therapeutic indices compared to previously reported QACs.
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Key words
antiseptics,quaternary ammonium compounds,methicillin-resistant Staphylococcus aureus (MRSA),bisQACs
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