. Author manuscript; available in PMC: 2010 Jul 9.

Published in final edited form as: J Med Chem. 2009 Jul 9;52(13):4038–4053. doi: 10.1021/jm900356n

Table 5.

Activity of New 5-NIs against Mz-Resistant G. lamblia

		activity against G. lamblia 713,^a pEC₅₀ (mean ± SE)		activity against G. lamblia 106,^a pEC₅₀ (mean ± SE)		EC₅₀(Mz^R)/EC₅₀(Mz^S)^b
group^c	name	Mz^S	Mz^R	Mz^S	Mz^R	G. lamblia 713	G. lamblia 106
	Mz	5.83 ± 0.08	4.35 ± 0.12	5.40 ± 0.10	4.59 ± 0.08	30.20	6.46
A	9	6.64 ± 0.23	5.89 ± 0.02	6.69 ± 0.31	6.37 ± 0.24	5.59	2.13
	11	7.49 ± 0.09	6.90 ± 0.12	7.37 ± 0.38	6.94 ± 0.11	3.95	2.73
	15	7.44 ± 0.10	6.84 ± 0.10	7.14 ± 0.08	6.59 ± 0.22	4.06	3.52
	19	7.59 ± 0.01	6.91 ± 0.09	7.51 ± 0.27	7.03 ± 0.10	4.76	3.07
B	10	7.74 ± 0.10	6.93 ± 0.14	7.38 ± 0.18	6.55 ± 0.43	6.40	6.81
	33	6.74 ± 0.09	6.32 ± 0.51	6.67 ± 0.23	5.54 ± 0.23	2.62	13.67
C	12	8.09 ± 0.46	7.04 ± 0.39	7.14 ± 0.17	6.70 ± 0.21	11.43	2.78
	23	7.49 ± 0.09	6.15 ± 0.12	7.19 ± 0.20	6.70 ± 0.14	22.00	3.11
	24	6.46 ± 0.18	5.34 ± 0.34	6.27 ± 0.27	5.91 ± 0.19	13.22	2.28
	28	7.29 ± 0.21	5.93 ± 0.02	7.06 ± 0.15	6.60 ± 0.14	22.96	2.84
other	5	7.69 ± 0.10	6.28 ± 0.20	7.26 ± 0.24	6.40 ± 0.14	25.98	7.20
	13	7.52 ± 0.27	6.94 ± 0.16	7.22 ± 0.13	6.60 ± 0.30	3.77	4.22
	29	7.69 ± 0.10	6.31 ± 0.19	7.45 ± 0.28	6.44 ± 0.09	23.95	10.32
	31	7.61 ± 0.61	5.98 ± 0.06	7.04 ± 0.03	6.41 ± 0.06	42.93	4.25
	36	6.76 ± 0.15	5.29 ± 0.03	6.29 ± 0.16	5.51 ± 0.11	29.51	6.00
	40	6.99 ± 0.16	5.30 ± 0.07	6.76 ± 0.13	5.59 ± 0.18	49.25	14.73

pEC₅₀ was determined for the respective Mz-sensitive (Mz^S) and Mz-resistant (Mz^R) lines of G. lamblia. Data are mean ± SE of three separate experiments.

The ratio of EC₅₀ in the Mz-resistant line to EC₅₀ in the isogenic Mz-sensitive line (“Mz resistance ratio”) is a measure of the ability of a compound to overcome Mz resistance in the respective G. lamblia lines.

Group refers to the Mz resistance groups depicted in Figure 3A.