TABLE 5.
Toxicities and antileishmanial activities of dimeric complexes of the B seriesa
| Compound | R1 | Log P | Log S | Pa | Toxicity (IC50, μM) | Antileishmanial activity (IC50, μM)
|
||
|---|---|---|---|---|---|---|---|---|
| Promastigotes | Amastigotes | SI | ||||||
| B28 | NH2 | 4.82 | −7.95 | 0.757 | 8.9 | 5.2 | Toxic | |
| B16 | NH2 | 5.61 | −7.88 | 0.753 | 127.4 | 1.3 | 0.8 | 159.2 |
| B29 | NH2 | 6.55 | −7.78 | 0.753 | 8.1 | 8.8 | Toxic | |
| B12 | Cl | 6.58 | −9.26 | 0.709 | 125.1 | 24.1 | 10.3 | 12.1 |
| B11 | Cl | 7.22 | −9.17 | 0.706 | 159.3 | 60.2 | 56.2 | 2.8 |
| B13 | Cl | 7.89 | −9.04 | 0.706 | 114.4 | 115.3 | 118.2 | |
a
Log P, lipophilicity; log S, solubility in water; Pa, predicted values for antileishmanial activity; SI, ratio between antileishmanial activity on amastigotes and toxicity.