Table 1.

SAR of the Methylene-3,4-dioxybenzoyl Moiety

		MIC50 (μM)
Compound	R	BioA-UEa	BioA-OEb	WT-biotinc	WT+biotind
6		0.4 (1.7)e	31.1 (>50)e	5.6 (23.4)e	>50 (>50)e
7		10.4	>50	>50	>50
8		21.1	>50	>50	>50
9		1.9	17.7	10.2	10.7
10		>50	>50	>50	>50
11		18.3	>50	28.6	39.1
12		0.5	7.5	5.1	30.1
13		>50	>50	>50	>50
14		14.6	>50	>50	>50
15		>50	>50	>50	>50
16		11.3	>50	>50	>50
17		>50	>50	>50	>50
18		>50	>50	>50	>50
19		10.6	47.6	8.7	6.2
20		>50	>50	>50	>50

^aMinimum inhibitory concentration (MIC) that results in 50% inhibition against the Mtb BioA underexpression strain.

^bMIC that results in 50% inhibition against the Mtb BioA overexpression strain.

^cMIC that results in 50% inhibition against Mtb H37Rv without supplemental biotin.

^dMIC that results in 50% inhibition against Mtb H37Rv with 1 μM supplemental biotin.

^eMIC that results in 90% inhibition.