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. 2017 Jul 10;8(8):886–891. doi: 10.1021/acsmedchemlett.7b00230

Table 1. In Vitro Antitrypanosomal Evaluation of N-Benzyl-2-thiohydantoins Derivatives (SAR R1–R2).

graphic file with name ml-2017-00230z_0006.jpg

compd R1 R2 T.brucei EC50 (nM)a
1 4-OMe 3-Cl 346
14 4-OMe H >10000
15 3-Cl H >20000
16 H H >10000
17 3-OMe H >10000
18 4-Cl H >10000
19 2-Cl H >20000
20 5-Cl 2-OMe >10000
21 4-CF3 3-Cl >10000
22 4-F 3-Cl >10000
23 5-Cl 2-F >10000
24 4-F H >10000
25 3-CF3 5-CF3 >10000
26 4-N(Me)2 H 1500
27 4-isoPr H >10000
28 4-OH H >10000
29 4–C(O)Me H >10000
30 4-COOH H >10000
31 4-OMe 2-OMe 637
32 4-OMe 3-OMe 161
33 4-OMe, 5-OMe 3-OMe >10000
34 4-N(Me)2 3-Cl 16
35 4-N(Me)2 3-F 125
36 4-N(Me)2 3-OMe 13
37 4-OMe 3-N(Me)2 431
a

Concentration of compound required to inhibit growth by 50% (EC50) in T. bruceibrucei strain BF427. Pentamidine isethionate was included as a control for all of the T. brucei EC50 assays with average ± SEM: 1.15 ± 0.09 nM (n = 32).