Table 1.

Results of antimycobacterial and cytotoxicity assays.

Compounds	R1	R2	ClogPa	MICb (μg/mL)	${\text{IC}}_{50}^{\text{c}}$ (μg/mL)	SId (IC50/MIC)
V	H	/	/	>50	/	/
VI	H	H	/	6.25	/	/
2a	H	H	−0.01	6.25	143.6	23
2b	H	-CH3	0.49	12.5	/	/
2c	H	-OMe	−0.09	12.5	/	/
2d	H	-F	0.14	3.13	122.8	39.2
2e	H	-Cl	0.71	3.13	115.7	37
2f	H	/	−1.54	25	/	/
2g	CH3	H	0.49	12.5	/	/
2h	CH3	-CH3	0.99	25	/	/
2i	CH3	-OMe	0.41	50	/	/
2j	CH3	-F	0.64	6.25	113.5	18.2
2k	CH3	-Cl	1.21	3.13	102.2	32.7
2l	OCH3	H	0.26	100	/	/
2m	OCH3	-CH3	0.76	100	/	/
2n	OCH3	-OMe	0.18	200	/	/
2o	OCH3	-F	0.40	50	/	/
2p	OCH3	-Cl	0.97	50	/	/
2q	F	H	0.29	6.25	126.4	20.2
2r	F	-CH3	0.79	12.5	/	/
2s	F	-OMe	0.21	25	/	/
2t	F	-F	0.43	1.56	100.9	64.7
2u	F	-Cl	1.00	1.56	91.2	58.5
2v	Cl	H	0.86	3.13	118.8	38
2w	Cl	-CH3	1.36	6.25	125.3	20
2x	Cl	-OMe	0.78	12.5	/	/
2y	Cl	-F	1.00	1.56	106.8	68.5
2z	Cl	-Cl	1.57	1.56	94.6	60.6
RMPe	/	/	/	0.125	/	/

^aCalculated by SYBYL-X 2.0 (Tripos, Inc.).

^bActual minimum inhibitory concentration (MABA assay).

^cMeasurement of cytotoxicity in VERO cells.

^dSelectivity index.

^eRifampicin.