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. Author manuscript; available in PMC: 2012 Feb 9.
Published in final edited form as: Eur J Med Chem. 2010 Jul 24;45(10):4682–4686. doi: 10.1016/j.ejmech.2010.07.030

Table 1.

Evaluation of 1a–l and 2 against M. tuberculosis H37Rva.

Compound Substituents in 1
IC50 (μM) IC90 (μM) log Pb
R1, R2, R3
1a H 3.88 6.12 1.44
1b 4-OCH3 23.1 40.2 1.39
1c 3,4-(OCH3)2 9.15 17.2 1.27
1d 3,4,5-(OCH3)3 6.88 11.9 1.03
1e 3,4-OCH2O 19.7 35.8 1.57
1f 4-CH3 5.58 9.44 1.91
1g 4-Cl 2.64 4.12 1.97
1h 3,4-Cl2 1.03 1.53 2.45
1i 4-Br 3.71 >250 2.34
1j 4-F 5.83 10.7 1.45
1k 4-NO2 >250 >250 1.22
1l 3-NO2 2.18 2.39 1.35
2 – 6.83 7.89 −0.90
a

The minimal inhibitory concentration to inhibit the growth of M. tuberculosis H37Rv of isoniazid is 0.18–0.36 μM and for rifampin, the figure is 0.02–0.15 μM [33].

b

The log P values were obtained using a free software package [36].