Table 1. In vitro screening data against three different trypanosomatids.

	All values as μM							Comp. Typee
Compound	T.b.rhodesiensea		T. cruzib		L. donovani axen. c		Cytotox. L6d
	IC-50	SI	IC-50	SI	IC-50	SI	IC-50
1	0.611	34	0.140	147	35.37	1	20.52	Nitro-Trz
2	0.134	74	0.151	66	10.15	1	9.935	Nitro-Trz
3	0.996	0	0.996	0	9.09	0	0.308	Nitro-Im
4	0.601	3	0.926	2	14.77	0	1.675	Nitro-Im
5	1.397	18	1.041	24	54.35	0	24.95	Nitro-Im
6	1.872	36	3.508	19	39.06	2	66.83	Nitro-Im
7	3.455	9	2.097	15	68.29	0	31.56	Nitro-Im
8	3.922	22	1.973	45	10.11	9	87.82	Nitro-Im
9	2.756	12	3.628	9	6.17	5	32.46	Nitro-Im
10	15.16	>16	4.28	>55	20.05	>12	>236.5	Nitro-Im
11	10.271	>28	7.081	>41	>95.69	∼3	>287.0	Nitro-Im
12	11.782	>23	41.82	>7	98.07	>3	>274.7	Nitro-Im
13	2.257	7	0.968	17	3.63	5	16.48	Nitro-Im
14	15.46	1	9.67	1	12.43	1	11.71	Nitro-Im
15	0.621	6	30.12	0	0.516	8	3.91	Nitro-Im
16	0.309	463	0.607	236	45.78	3	143.22	Nitro-Trz
17	0.193	708	0.14	976	64.49	2	136.6	Nitro-Trz
18	0.117	973	0.305	373	136.56	1	113.83	Nitro-Trz
19	21.82	>14	92.14	>3	>298.5	∼1	>298.5	Trz
20	1.417	68	1.48	66	9.48	10	96.99	Nitro-Trz
21	0.562	137	1.74	44	8.69	9	77	Nitro-Trz
22	2.191	>131	33.7	>8	>95.39	∼3	>286	Nitro-Trz
23	2.22	60	1.031	129	182.29	1	132.67	Nitro-Trz
24	0.435	220	0.46	208	>275.5	0	95.77	Nitro-Trz
25	0.882	8	15.6	0	6.53	1	7.16	Nitro-Trz
26	13.8	10	24.48	6	>69.36	∼2	139.65	Nitro-Im
27	23.04	>7	3.77	>46	6.49	>27	>172.25	Nitro-Im
28	21.57	4	8.02	10	4.27	19	79.62	Nitro-Im
29	7.84	18	0.169	816	11.07	12	137.9	Nitro-Trz
30	8.17	10	1.96	40	4.87	16	78.79	Nitro-Trz
31	32.30	>7	123.40	>2	172.25	>1	>223.6	Trz
32	8.56	16	6.05	23	80.28	2	137.03	Nitro-Im
33	14.23	7	4.67	20	18.67	5	93.6	Nitro-Im
34	1.05	136	0.311	460	63.81	2	143.13	Nitro-Trz
35	0.917	78	0.358	200	9.58	7	71.62	Nitro-Trz
36	0.463	99	0.32	144	9.33	5	46	Nitro-Trz
37	3.61	34	0.32	383	158.7	1	122.41	Nitro-Trz
38	0.271	339	0.145	634	0.348	264	91.88	Nitro-Trz
39	15.30	>13	20.72	>9	>191.49	∼1	>191.49	Nitro-Im
40	1.38	>140	0.34	>562	58.15	>3	>191.08	Nitro-Trz
41	1.2	99	0.412	287	44.45	3	118.37	Nitro-Trz
42	5.33	10	0.04	1320	25.92	2	52.79	Nitro-Trz
Melarsoprol	0.01*
Benznidazole			1.35*
Miltefosine					0.44*
	active,
	moderate activity
	active, but cytotoxic, low specificity
	compounds have been previously synthesized.19, 23, 29-31

^aSTIB 900 trypomastigotes;

^bTulahuen C4 amastigotes;

^cMHOM-ET-67/L82 amastigotes;

^dCytotoxicity measurements;

^eNitro-Trz: 3-nitro-1H-1,2,4-triazole; Nitro-Im: 2-nitro-1H-imidazole; Trz: not nitro triazole;

^*Median values from 43 measurements in parallel with each compound. SI = IC₅₀ in L6 cells / IC₅₀ in parasites.