Table 1 Activity of novel chemotypes against M. tuberculosis.

Chemotype	Molecule	% Inhibition¹		MTB²	HepG2³
Chemotype	Molecule	Run 1	Run 2	MIC (µM)	IC₂₀ (µM)
4-phenylpiperidine	4PP-1	100	99	6.3	> 80
Aminoarylpyridine	AAP	99	97	23	27
Acetyl indole	ACI-2	100	100	4.5	30
Acyl cyclic urea	ACU-1	98	98	7.6	65
Aminomethylquinoxaline	AMQ-5	98	99	7.8	2.0
Aminomethylthiazole	AMT-1	98	96	35	34
Aminopyridylpyrimidine	APDP-1	99	100	10	0.028
Aminophenyltetrazoles	APT	99	99	6.9	0.47
Benzimidazolyl cyanoimines	BCI-2	100	100	9.6	0.85
Benzoxazinones	BOZ	99	100	4.8	37
Benzotriazinylthiazoles	BTT	100	100	4.8	37
Diaminopyrimidines	DAP	99	99	0.7	0.83
Furanylaminosulfones	FAS	100	100	9.5	2.0
Hydrophobic urea	HBU-1	100	100	4.2	8.2
Hydroxyureas	HDU-2	99	100	19	42
Phenylcyclobutanecarboxamides	PCB-1	100	100	6.9	33
Pyrazolylpyrrolopyridines	PDPO-1	99	96	23	2.8
Pyridylpyrimidines	PPP-1	100	98	38	4.3
Phenyltetrazolones	PTZ-3	96	6	5.2	26
Pyrrolotriazines	PYT	100	98	11	23
Pyrazoloindoles	PZI	98	98	9.3	15
Pyrazolylpyrimidines	PZP-3	98	98	4.5	47
Thienylpyrazolylthiazoles	TPT	99	99	7.1	> 80
Thiazolyl Furans	TZF	99	99	18	> 80

We determined the MIC of a representative molecule for each chemotype.
¹% Inhibition of M. tuberculosis growth after 5 days in the primary screen (duplicated runs).
²MIC is the concentration required to achieve 90% inhibitions of growth of M. tuberculosis in aerobic culture (n ≥ 2).
³IC₂₀ is the concentration required to achieve 20% inhibition of HepG2 cells (n = 2).

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