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. Author manuscript; available in PMC: 2009 Sep 14.
Published in final edited form as: Biochemistry. 2005 Dec 20;44(50):16574–16583. doi: 10.1021/bi0518186

Table 1.

LpxC inhibition and/or antibacterial activity of selected compounds.

Compound % inhibition EcLpxC % inhibition AaLpxC G17S
mm killing c
R477
mm killing c
PAO1
mm killing c
Time Dependent d
L-161,240 a 96 3 30 19 < 6 no
TU-514 a 50 > 99 < 6 < 6 < 6 no
CHIR-090 b 98 98 38 36 34 yes

tobramycin Not tested Not tested 28 26 24 N/A
ciprofloxacin Not tested Not tested 37 35 40 N/A
a

Tested at 1 μg/mL in the assay at pH 7.4

b

Tested at 0.5 μg/mL (1.15 μM) in the assay at pH 7.4

c

Tested at 20 μg/disc (disc diameter = 6 mm)

d

Tested by preincubation of AaLpxC (3.3 nM) with 0.02 μg/mL inhibitor