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. 2013 Dec 6;5(1):89–93. doi: 10.1021/ml400412x

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