Table 5. Antileishmanial Activity of Compounds 22–31.
| MRC5a |
HLM | HamLM | ||||||
|---|---|---|---|---|---|---|---|---|
| compound | R1 | R2 | intramacrophage L. infantum amastigote EC50 (μM)a | PMMa CC50 (μM) | CC50 (μM) | SIb | Clint (μL/min/mg) | |
| 22 | H | 2-pyridyl | 1.7 | >64 | 44.8 | 30 | <11.9 | 18 |
| 23 | CH3 | 2-pyridyl | 1.8 | >64 | >64 | >39 | <11.9 | <11.9 |
| 24 | CH3 | phenyl | 37 | >64 | >64 | >1.7 | <11.9 | n.d. |
| 25 | CH3 | 2-pyridyl-6-OMe | 0.8 | 32 | >64 | >80 | 23 | 40 |
| 26 | CH3 | 2-pyridyl-6-Me | 6.4 | >64 | >64 | >10 | n.d. | n.d. |
| 27 | CH3 | 3-pyridyl | 38 | >64 | >64 | >1.8 | n.d. | n.d. |
| 28 | CH3 | 2-pyridyl | 0.5 | 49 | 18 | 37 | <11.9 | 40 |
| 29 | CH3 | 2-pyridyl | 1.7 | 29 | 45 | 18 | <11.9 | 82 |
| 30 | CH3 | 2-pyridyl | 0.6 | 32 | 2.3 | 4 | <11.9 | 88 |
| 31 | 2-pyridyl | 2.0 | >64 | >64 | >32 | 19 | 12 | |
a
Geometric mean value of at least two independent tests.
b
Selectivity index representing the ratio of CC50/EC50; data are presented as the geometric mean value of ratios calculated using separate data from at least two independent tests. n.d., not determined.