Table 17.
Antitrypanosomal activity, metabolic stability and lipophilicity of benzimidazoles 21g-j.
| |||||
|---|---|---|---|---|---|
| Compound | R | T. cruzi IC50 a Tulahuen CL2 Strain | SIb | MLM CIint µg/min/mg | eLogD |
| 21g |
|
2.6 ± 0.66 | >25 | 18 | 3.1 |
| 21h |
|
0.28 ± 0.30 | >231 | 27 | 3.1 |
| 21i |
|
0.23 ± 0.96 | 34 | 28 | 3.0 |
| 21j |
|
1.5 ± 3.19 | >42 | 25 | 2.9 |
| Benznidazole | 2.1 | nd | nd | nd | |
Note: aIC50: compound concentration that reduced the parasite load of 50%; bSI: selectivity index (CC50 MRC-5 /IC50 parasite); nd = not determined.