Skip to main content
. Author manuscript; available in PMC: 2015 Apr 1.
Published in final edited form as: ChemMedChem. 2014 Mar 11;9(4):776–791. doi: 10.1002/cmdc.201300429

Table 3.

Derivatives with heterocyclic B-rings.

Compound IC50 (nM)[a][c] MIC[b] (μg/mL) Slow-onset Residence time (min)
R
PT077 graphic file with name nihms-584957-t0014.jpg H 190 ± 12 3.13 No
PT164 -CN 308 ± 4.2 <0.39 Yes N.D.[d]
PT161 -F 40 ± 20 0.3125 Yes N.D.[d]
PT112 graphic file with name nihms-584957-t0015.jpg -NH2 69000 ± 700 50 N.D.[d]
PT115 -CN 890.6 ± 105.8 12.5 Yes >20
PT116 -COOH >12000 25 N.D.[d]
PT134 graphic file with name nihms-584957-t0016.jpg 238.8 ± 46.8 3.125 N.D.[d]
[a]

The half maximal inhibitory concentration (IC50) is the concentration of an inhibitor that is required for inhibition of 50% of the enzyme activity.

[b]

The minimum inhibitory concentration (MIC) is the lowest concentration of an inhibitor that is adequate to inhibit visible growth of bacteria.

[c]

IC50 values were determined at an enzyme concentration of 100 nM.

[d]

N.D. = Not determined.

IC50 and Ki values are average results from 3 independent experiments with standard deviation.