Table 1.

IC₅₀ Values against Purified Eis and KAN MIC Values against Mtb H37Rv and Mtb K204 in the Absence and Presence of the Compounds at the Specified Concentrations

compd no.	Ar	X	IC50 (μM)a	concentration tested (μM)b	H37Rv MICKAN (μg/mL)c	K204 MICKAN (μg/mL)d
					1.25	10
29	p-Br-Ph	Me	0.08 ± 0.02	8	≤1.25	2.5
30	p-Br-Ph	H	6.2 ± 1.3	100	≤1.25	5
31	Ph	Me	5.8 ± 1.8	100	≤1.25	5
32	Ph	H	>200	100	≤1.25	10
33	p-iPr-Ph	Me	0.25 ± 0.06	25	≤1.25	2.5-5
34	p-iPr-Ph	H	10.6 ± 2.5	100	≤1.25	5
35	p-Cl-Ph	Me	0.100 ± 0.045	10	≤1.25	2.5
36	o-OMe-Ph	Me	>200	100	≤1.25	10
37	m-F-Ph	Me	3.0 ± 0.7	30	≤1.25	5
38	m-Br-Ph	Me	0.056 ± 0.004	5.6	≤1.25	2.5
39	m-OMe-Ph	Me	5.8 ± 1.2	100	≤1.25	≤1.25
40	3,5-di-OMe-Ph	Me	7.4 ± 3.3	100	≤1.25	5-10
41	m-Me-Ph	Me	0.37 ± 0.09	37	≤1.25	2.5-5
42	m-Et-Ph	Me	0.027 ± 0.012	2.7	≤1.25	5-10
43	m-iPr-Ph	Me	0.23 ± 0.03	23	≤1.25	2.5-5
44	m-nBu-Ph	Me	0.7 ± 0.3	70	≤1.25	5-10
45	m-tBu-Ph	Me	27 ± 8	100	≤1.25	5-10
46	2-naphthyl	Me	0.00024 ± 0.00010	100	≤1.25	≤1.25
47	4-OMe-2-naphthyl	Me	0.30 ± 0.08	100	≤1.25	10

^aIC₅₀ values and standard errors for inhibition of purified Eis enzyme.

^bCompounds were tested at concentrations that were either 100-fold higher than their IC₅₀ or at 100 μM if the IC₅₀ value could not be achieved while keeping the DMSO concentration at ≤1% in test wells. At these concentrations, the compounds did not inhibit the growth of Mtb H37Rv or that of Mtb K204 when tested in the absence of KAN.

^cAnti-TB activity of KAN against Mtb H37Rv.

^dAnti-TB activity of KAN against Mtb K204.