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. Author manuscript; available in PMC: 2011 Jun 15.

Published in final edited form as: Bioorg Med Chem Lett. 2010 May 18;20(12):3537–3539. doi: 10.1016/j.bmcl.2010.04.126

Table 1.

Selected NTZ-head group Analogue Activity

	MIC’s (μM)
Analogue	H. pylori	C. jejuni	C. difficile	PFOR Inhibition [Drug] = 40 μM (%)

Nitazoxanide (1)	13.0	39.1	0.8	54 ± 7
3a	0.5	2.1	8.2	70
3b	1.3	3.0	32.1	53 ± 8
3c	3.5	4.7	0.4	47
3d	2.9	2.9	1.0	50
3e	0.8	12.5	2.1	56
6a	0.9	3.6	28.8	63^a
6b	8.8	7.0	>28.2	59
6c	5.7	34.1	>22.7	27 ± 2
6d	6.9	13.8	>13.8	51
9a	2.6	0.9	27.8	80 ± 8^a
9b	1.3	0.9	27.3	55
9c	0.5	2.1	4.2	47
9d	2.5	1.0	20.0	77
9e	2.6	0.4	3.5	66 ± 13^a

^a

Complex pattern of inhibition with two different rates.