Table 3.
In vitro activity of aaptamine and derivatives a (1, 2, 5-30) against chloroquine sensitive and resistant malarial strains Plasmodium falciparum (Pf-D6, Pf-W2) and Mycobacterium tuberculosis (Mtb)
| Anti-malarial (IC50, μM)a,c |
|||
|---|---|---|---|
| Compound | Pf-D6 | Pf-W2 | Mtb MIC (μM)b,c |
| 1 | NA | NA | NA |
| 2 | 5.3 | NA | NA |
| 5 | 8.2 | 11.9 | NA |
| 6, 7 | NA | NA | NA |
| 8 | 3.1 | 8.6 | NA |
| 9 | 7.4 | 7.4 | NA |
| 10-12 | NA | NA | NA |
| 13 | 13.4 | NA | NA |
| 14 | 11.4 | NA | NA |
| 15 | 2.3 | 2.3 | NA |
| 16 | 0.6 | 0.9 | 4.1 |
| 17 | 2.3 | 2.9 | 15.2 |
| 18 | 2.4 | 2.5 | 9.8 |
| 19 | 1.9 | 2.7 | 6.8 |
| 20 | 1.2 | 2.0 | 6.8 |
| 21 | 2.5 | 3.9 | 5.1 |
| 22 | NA | NA | 28.9 |
| 23 | 8.2 | NA | – |
| 24 | 5.4 | 5.4 | NA |
| 25 | 6.2 | 6.9 | – |
| 26 | NA | NA | 16.1 |
| 27 | 0.4 | 0.5 | NA |
| 28 | 0.4 | 0.5 | 11.2 |
| 29 | NA | NA | – |
| 30 | 0.6 | 0.2 | – |
a
Anti-malarial control IC50: (artemesinin) 0.1 and 0.05 μM respectively.
b
Anti-Mtb control IC50: (rifampin) 0.1 μM.
c
NA= >8.4 μM; Mtb NA= >47.8 μM; NR = Not active in primary screening