Paper
Organic & Biomolecular Chemistry
and was allowed to stand for 10 min, then 125 μL from
each well was transferred to a polystyrene microtiter plate and
the OD540 of each well was measured and the water lanes
were subtracted out. The percentage of biofilm inhibition was
calculated.
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Conclusions
In summary, an analogue library of the bacterial metabolite 2b
was constructed in a matrix fashion. Testing of the compounds
revealed a single analogue (3j) that was potent against several
strains of medically relevant MRSA. Compound 3j inhibited
bacterial biofilm formation by 50.8–93.9% at 200 μM against
MRSA strains respectively and low to moderate micromolar
IC50 values ranging from 15.7 4.0 μM–215.0 7.6 μM. The
ease of synthesis and simplistic nature of 3j make it an attrac-
tive option for bacterial biofilm control of MRSA. We are cur-
rently testing these analogues for their ability to potentiate
cancer chemotherapeutics to determine if there is a substan-
tial correlation between these two apparently disparate
activities.
Acknowledgements
16 C. Bunders, J. Cavanagh and C. Melander, Org. Biomol.
Chem., 2011, 9, 5476–5481.
The authors would like to thank the V foundation, the
National Institutes of Health (GM055769 and DE022350), and
Faculty of Science, Mahidol University for their generous
support of this work.
17 S. A. Rogers, D. C. Whitehead, T. Mullikin and
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