Table 1.

In vitro activity of compounds 1a–p.

1a–i R1=CF3				1j–p R1=NO2
Code	R2	Residual activity at 100 µM (%)	MbtI IC50 (µM)*	Code	R2	Residual activity at 100 µM (%)	MbtI IC50 (µM)*
1a	Cl	6.1 ± 2.5	28.5 ± 2.6	I**	Cl	11.3 ± 4.2	17.9 ± 3.2
1b	F	6.1 ± 1.1	27.6 ± 7.3	1j	F	32.1 ± 2.4	–
1c	Br	38.0 ± 3.7	–	1k	Br	26.4 ± 4.8	–
1d	OH	16.8 ± 2.7	35.9 ± 10.3	1l	OH	13.9 ± 4.0	29.8 ± 4.2
1e	CH3	19.3 ± 2.2	31.5 ± 9.6	1m	CH3	13.2 ± 5.8	28.5 ± 1.5
1f	NH2	13.1 ± 2.4	34.6 ± 10.9	1n	NH2	13.5 ± 3.8	24.2 ± 5.4
1g	CN	5.7 ± 1.5	18.5 ± 3.2	1o	CN	5.0 ± 1.9	24.4 ± 5.9
1h	CF3	3.9 ± 1.7	13.1 ± 2.0	1p	CF3	25.1 ± 3.7	41.8 ± 5.3
1i	m-CF3	64.3 ± 4.5	–	–	–	–	–

*Only for compounds with residual activity ≤25%; **new fluorimetric assay value determined for the sake of comparison.