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. Author manuscript; available in PMC: 2015 Aug 1.
Published in final edited form as: Bioorg Med Chem Lett. 2014 May 28;24(15):3493–3498. doi: 10.1016/j.bmcl.2014.05.062

Table 1.

In vitro evaluation of compounds 2, 6-12 against H37Rv Mtb in GAST media, 7H12 media and LORA as well as toxicity to VERO cells (IC50 in μM).

Compound Mol Wt Calcd
Clog Pa 		MIC mean +/− against replicating Mtb in
medium:		 LORA
(μM)		 VERO
IC50
(μM)
GAS (μM) GAS (μg/mL) 7H12 (μM)
graphic file with name nihms-601528-t0007.jpg 279.34 3.60 0.11±0.008 0.031±0.002 0.49±0.004 >128 >128
graphic file with name nihms-601528-t0008.jpg 280.32 2.60 1.27±0.22 0.36±0.06 6.95±0.15 >128 >128
graphic file with name nihms-601528-t0009.jpg 280.32 2.26 63.8±1.9 17.9±0.5 >128 >128 24.7
graphic file with name nihms-601528-t0010.jpg 278.35 3.73 43.8±1.2 12.2±0.3 >128 >128 >128
graphic file with name nihms-601528-t0011.jpg 265.31 4.02 40.8±3.3 10.8±0.9 >128 >128 >128
graphic file with name nihms-601528-t0012.jpg 267.31 2.85 101±6.0 27±1.6 >128 >128 >128
graphic file with name nihms-601528-t0013.jpg 281.31 2.20 126±2.9 35.4±0.8 >128 >128 >128
graphic file with name nihms-601528-t0014.jpg 279.34 3.61 70±8.9 19.6±2.5 >128 >128 >128
graphic file with name nihms-601528-t0015.jpg 822.95 6.04 0.11 0.09 0.06 2.6 113
graphic file with name nihms-601528-t0016.jpg 359.26 2.62 0.12 0.04 0.09 4.9 >128

SD, standard deviation; MIC, minimum concentration required to inhibit growth by >90%; GAS, Glycerol-alanine-salts media; 7H12, Middlebrook7H9 broth base media with BSA, casein hydrolysate, catalase, palmitic acid; LORA, Low oxygen recovery assay using the H37Rv luxAB Mtb luminescence strain; VERO, African green monkey kidney cell line to evaluate toxicity. Values reported are the average of three individual measurements.

a

Calculated Clog P by ChemDraw version 12.0