Table 2.
compd | R1 | R2 | R3 | Pf DXR IC50 [μM] |
---|---|---|---|---|
1a | 1.087 ± 0.064 | |||
1b | 0.511 ± 0.0535 | |||
2 | Na/H | H | CH3 | 0.202 ± 0.01535 |
3 | POM | H | CH3 | 0.018 ± 0.00235 |
12a | Na/H | H | H | 0.019 ± 0.002 |
12b | Na/H | H | CF3 | 113.3 ± 22.4 |
12c | NH4 | H | OCH3 | 28.6 ± 5.0 |
16d | Na/H | CH(CH3)Ph | CH3 | 1.2 ± 0.1 |
16e | Na/H | CH2(4-iprPh) | CH3 | 1.1 ± 0.0 |
16f | Na/H | CH2(2-naphthyl) | CH3 | 26.1 ± 1.1 |
16g | Na/H | CH2(4-biphenyl) | CH3 | 2.3 ± 0.4 |
18a | POM | H | H | 0.013 ± 0.002 |
18b | POM | H | CF3 | 14.3 ± 2.5 |
18c | POM | H | OCH3 | 23.7 ± 6.6 |
19e | POM | CH2(4-iprPh) | CH3 | 55.2 ± 1.9 |
19f | POM | CH2(2-naphthyl) | CH3 | 50.5 ± 1.1 |
19g | POM | CH2(4-biphenyl) | CH3 | 44.1 ± 1.1 |
Pf = P. falciparum; IC50 = concentration giving 50% inhibition of Pf growth