10.1002/cmdc.201800622
ChemMedChem
FULL PAPER
Inspection of the bioactivity profile of the 21 prepared antiseptics, lysing the cell, and if this varies by QAC architecture; such
categorized by their parent core structure, indicates some clear
trends. First and foremost, we see another reassertion that
bisQAC antiseptics demonstrate superior antimicrobial activity
as compared to their monoQAC counterparts. BAC and CPC,
despite strong activity against the three strains of
staphylococcus, show relatively weak activity (≥125 µM) versus
E. faecalis as well as P. aeruginosa; even more dramatic
differentiation (up to 250X) is seen when comparing pip-12,0
and pip-12,12, as well as in DABCO-12,0 vs DABCO-12,12.
Also in support of historical precedent, the chain length of
the non-polar side chains of the amphiphile are crucial for
antimicrobial activity; the possession of ~12 carbons in the alkyl
chain, or 12-13 atom side chains for the amide containing
experiments are precedented[22] and represent a future direction
for our groups.
Acknowledgements
This work was funded by the National Institute of General
Medical Sciences (GM119426 to W.M.W.) and Villanova
University.
Keywords: antiseptics · bisQAC · methicillin-resistant
Staphylococcus aureus (MRSA) · quaternary ammonium
compounds · benzalkonium chloride
antiseptics, are optimal for antimicrobial activity.
Further,
amphiphiles with longer side chains (i.e., ≥14 carbons) show
diminished water solubility.
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In regards to the effects of structural rigidity of the core of
the bisQAC, results were not as anticipated, as we expected that
maximal flexibility would allow for facile entry of the non-polar
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