Table 2. SAR Analysis of Aryl Substituents.
cmpd | R1 | R2 | R3 | Pf 3D7 IC50 (μM) | cLogP |
---|---|---|---|---|---|
10a | cHex | 3-OMe | 3-OMe | 0.768 | 3.9 |
(±)-10b | cHex | 4-OMe | H | 0.533 | 4.1 |
(±)-10c | cHex | 3-OMe | H | 0.917 | 4.1 |
10d | cHex | 4-OCF3 | 4-OCF3 | 2.20 | 7.1 |
10e | cHex | 4-OEt | 4-OEt | 0.466 | 4.6 |
10f | cHex | 4-Me | 4-Me | 1.26 | 5.3 |
10g | cHex | 3-Me | 3-Me | 0.533 | 5.3 |
10h | cHex | 4-Cl | 4-Cl | 1.07 | 5.5 |
10i | cHex | 3-Cl | 3-Cl | 1.06 | 5.5 |
(±)-10j | cHex | 3-Ph | 4-OMe | 1.49 | 5.7 |
(±)-10k | cHex | 3-(3-pyr) | 4-OMe | 0.595 | 4.5 |
(±)-10l | cHex | 3-(3-pyr) | 3-OMe | 0.787 | 4.5 |
(±)-10m | cHex | 3-(3-pyr) | H | 0.75 | 4.7 |
(±)-10n | cHex | 3-(2-pyr) | 4-OMe | 1.81 | 4.9 |
(±)-10o | cHex | 3-(4-pyr) | 3-OMe | 0.318 | 4.5 |
10p | cHex | 3-(3-pyr) | 3-(3-pyr) | 0.725 | 5.1 |
(±)-10q | cHex | 3-OPh | H | 0.424 | 5.7 |
(±)-10r | cHex | 3-OBn | H | 0.641 | 5.8 |
(±)-11 | Me | 3-(3-pyr) | H | 6.88 | 5.8 |