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. 2017 Sep 18;2(9):5873–5890. doi: 10.1021/acsomega.7b00892

Table 3. SAR Studies of the Thiazole Region of 1.

graphic file with name ao-2017-00892q_0006.jpg

compound R1 R2 R3 MIC (μM) TC50 (μM)
45 H H OAc >20 >50
46 NO2 Me OH >20 5.2
47 COOMe H OH >20 >50
48 Me H N/A >20 12
49 CF3 H N/A 5.3 ± 0.20 0.8
50 NO2 Me N/A 1.5 ± 0.60 4.2
51 COOH H N/A >20 >50
52 H 2-pyridyl N/A >20 15
53 NO2 2-pyridyl N/A 8.5 ± 2.1 6.4
a

Compounds were tested for activity against M. tuberculosis. MIC (in μM) is the minimum concentration required to inhibit the growth of M. tuberculosis in liquid culture. MICs of active compounds are the average ± standard deviation of two independent experiments except where asterisked (N = 1).

b

Toxic concentration (TC50, in μM) is the concentration required to inhibit growth of Vero cells by 50%.