| L. donovani(GI50μM) |  | ||||||||
---|---|---|---|---|---|---|---|---|---|---|
Cpd | Y | R1 | R2 | R3 | R4 | R5 | R6 | Promastigotes | Intracellular amastigotes | ΜΦ J774.1 (GI50μM) |
1 | NO | H | Br | H | H | H |
| >3 μΜ | >3 μΜ | - |
2 | NO | H | Br | H | H | H |
| >3 μΜ | >3 μΜ | - |
3 | NO | H | Br | H | H | H |
| >3 μΜ | >3 μΜ | - |
4 | NO | H | Br | H | H | H |
| 1.15 ± 0.06 | - | 1.5 ± 0.07 |
5 | NO | H | Br | H | H | H |
| 0.9 ± 0.11 | - | 1.5 ± 0.08 |
6 | NO | H | Br | H | H | H |
| >3 μΜ | >3 μΜ | - |
7 | NO | H | Br | H | H | H |
| >3 μΜ | >3 μΜ | > 10 |
8 | NO | H | Br | H | H | H |
| >3 μΜ | >3 μΜ | >10 |
9 | NO | H | Br | H | H | H |
| >3 μΜ | >3 μΜ | >10 |
10 | NO | H | Br | H | H | H |
| >3 μΜ | >3 μΜ | > 10 |
11 | NO | H | Br | H | H | H |
| 0.75 ± 0.05 | 0.59 ± 0.07 | 6.25 ± 0.08 |
12 | NO | H | Br | H | H | H |
| 0.65 ± 0.09 | 0.80 ± 0.12 | 2.60 ± 0.05 |
13 | NO | H | Br | H | H | H |
| 0.82 ± 0.21 | 0.85 ± 0.16 | 2.41 ± 0.11 |
14 | NO | H | Br | H | H | H |
| 1.40 ± 0.10 | 1.71 ± 0.09 | 9.20 ± 0.15 |
15 | NO | H | Br | H | H | H |
| 1.50 ± 0.14 | 2.44 ± 0.17 | 6.00 ± 0.08 |
16 | NO | H | Br | H | H | H |
| 0.76 ± 0.03 | 1.54 ± 0.11 | 5.93 ± 0.04 |
17 | NO | H | Br | H | H | H |
| 0.76 ± 0.04 | 1.22 ± 0.06 | 10.00 ± 0.02 |
18 | NO | H | Br | H | H | H |
| >3 μΜ | >3 μΜ | - |
19 | NO | H | Br | H | H | H |
| >3 μΜ | >3 μΜ | - |
20 | O | H | H | Br | H | H | - | >3 μΜ | >3 μΜ | - |
21 | NO | H | H | Br | H | H | H | >3 μΜ | >3 μΜ | > 10 |
22 | O | H | H | Br | COOH | H | - | >3 μΜ | >3 μΜ | - |
23 | NO | H | H | Br | COOH | H | H | >3 μΜ | >3 μΜ | - |
24 | O | H | H | Br | H | COOH | - | >3 μΜ | >3 μΜ | - |
25 | NO | H | H | Br | H | COOMe | H | >3 μΜ | >3 μΜ | - |
26 | NO | H | H | Br | H | COOH | H | >3 μΜ | >3 μΜ | - |
27 | NO | H | H | CF3 | H | H | H | >3 μΜ | >3 μΜ | - |
28 | NO | H | H | CF3 | COOMe | H | H | >3 μΜ | >3 μΜ | - |
29 | O | H | H | CF3 | COOH | H | - | >3 μΜ | >3 μΜ | - |
30 | NO | H | H | CF3 | COOH | H | H | >3 μΜ | >3 μΜ | - |
31 | O | H | H | CF3 | H | COOH | - | >3 μΜ | >3 μΜ | - |
32 | NO | H | H | CF3 | H | COOMe | H | >3 μΜ | >3 μΜ | > 10 |
33 | NO | H | H | CF3 | H | COOH | H | >3 μΜ | >3 μΜ | - |
34 | O | H | H | CF3 |
| H | - | >3 μΜ | >3 μΜ | - |
35 | NO | H | H | CF3 |
| H | H | >3 μΜ | >3 μΜ | - |
6BIO | NO | H | Br | H | H | H | H | 0.85 ± 0.05 | 0.70 ± 0.10 | >25 |
5-Me-6-BIO | NO | CH3 | Br | H | H | H | H | 1.2 ± 0.2 | 1.0 ± 0.1 | >25 |
Amphotericin B | - | - | - | - | - | - | - | 0.10 ± 0.01 | 0.20 ± 0.02 | - |