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. Author manuscript; available in PMC: 2013 Oct 28.
Published in final edited form as: Curr Top Med Chem. 2012;12(7):766–796. doi: 10.2174/156802612799984571

Table 5.

MbtA Inhibitors: Aryl Domain SAR

graphic file with name nihms520750u2.jpg
Compound, R = KIapp (μM) MIC99 (μM) (iron-deficient) MIC99 (μM) (iron-rich)
graphic file with name nihms520750t16.jpg 51 OH 0.0066 ± 0.00015d 0.39 1.56
58 H 0.092 ± 0.007 12.5 50
59 F 0.038 ± 0.008 12.5 50
60 NH2 0.77 ± 0.12 > 200 > 200
61 NO2 7.32 ± 0.9 > 200 > 200
62 Cl 18.1 ± 1.7 > 200 > 200
graphic file with name nihms520750t17.jpg 63 3-Cl 0.061 ± 0.003 50 > 200
64 4-Cl 0.012 ± 0.0006 12.5 50
65 5-Cl 0.020 ± 0.0014 12.5 50
66 4-F 0.012 ± 0.0016 0.098 0.39
67 4-Br 0.021 ± 0.001 6.25–12.5 50
68 4-CH3 0.014 ± 0.0007 1.56 25
69 4-CF3 4.38 ± 0.44 > 200 > 200
70 4-NH2 0.040 ± 0.004 1.56 25
71 6-F 0.0073 ± 0.0006 0.78 3.13
graphic file with name nihms520750t18.jpg 72 0.137 ± 0.012 > 200 > 200
graphic file with name nihms520750t19.jpg 73 3.7 ± 0.5 > 200 > 200