. Author manuscript; available in PMC: 2010 Mar 12.

Published in final edited form as: J Med Chem. 2009 Mar 12;52(5):1329–1344. doi: 10.1021/jm801374t

Table 1.

Biological Activities of 2-position analogs of PA-824.

Number	Name	H37Rv MIC (µM)	H37Rv MAC (µM)	Rv3547^b k_cat/K_m (min⁻¹µM⁻¹)
1	PA-824	0.8	6.25 – 12.5	0.155
	2C-824^a	25	250	0.024
9	2-amino-824	0.8	125	0.243
10	2-N-formyl-824	3.2	25	0.065
11	2-acetamido-824	6.25	31.25	nd
12	2-N-Me-824	6.25	≥100	0.061
16	(R)-2S-824	0.8–1.6	25	0.146
17	2-SO-824	>100	50–100	ns
18	2-SO₂-824	>100	25	nd
19	(S)-2S-824	50	50 – 100	ns

reference ⁷.

ns = not a substrate, nd = not determined.