Table 2.
IC50 (µM) * | ||||||||
---|---|---|---|---|---|---|---|---|
Compd. | R1 | R2 | R3 | R4 | R5 | L. major promastigotes | L. donovani promastigotes | J774.1 |
14 | -H | -H | -Cl | -Cl | 65.6 | >100 | 58.9 | |
15 | -H | -H | -H | -H | 39.6 | 15.6 | 45.2 | |
16 | -H | -OCH3 | -H | -H | 60.9 | >100 | 42.6 | |
17 | -H | -Cl | -H | -Cl | 80.5 | >100 | 60.6 | |
18 | -H | -H | -H | -H | 64.3 | 51.2 | 46.0 | |
19 | -H | -H | -H | -H | 55.0 | >100 | 44.8 | |
20 | -H | -H | -H | -H | 53.1 | 79.7 | 44.8 | |
21 | -H | -H | -H | -H | 60.0 | >100 | 46.7 | |
22 | -H | -H | -H | -H | 67.0 | 28.7 | 44.5 | |
23 | -H | -H | -H | -H | >100 | 23.4 | >100 | |
24 | -H | -H | -H | -H | >100 | >100 | >100 | |
25 | -H | -H | -H | -H | >100 | 80.3 | 32.2 | |
26 | -H | -H | -H | -H | >100 | 41.9 | >100 | |
28 | -OAc | -OAc | -H | -H | 30.7 | - | 2.1 |
* Positive control: pentamidine 82 μM (L. major), 38.6 μM (J774.1); miltefosine: 36.2 μM (L. major), 56.5 μM (J774.1); amphotericin B 0.4 μM (L. donovani).