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. 2011 Jun 6;54(14):5116–5130. doi: 10.1021/jm2003359

Table 4. SAR Study of R3 Moiety.

graphic file with name jm2003359_0024.jpg

        IC50 a (nM)
compd R1 R2 R3 3D7 W2
21 α-Me-Ala 4F-Ph cyclohex- 9610 5980
22 α-Me-Ala 4F-Ph 3-pyridine 1413 3320
23 Gly 4F-Ph 3F-Ph 50 34
24 α-Me-Ala 3F-Ph 4F-Ph 50 71
25 Gly 4F-Ph 4Me-Ph 10 13
26 α-Me-Ala 4F-Ph 4Me-Ph 20 24
27 Gly 4F-Ph 4Cl-Ph 10 9
28 α-Me-Ala 4F-Ph 4Cl-Ph 30 24
29 Gly 4F-Ph 3F,4F-Ph 30 23
30 α-Me-Ala 4F-Ph 3F,4F-Ph 44 36
31 Gly 4F-Ph 3F,4Cl-Ph 3 4
32 α-Me-Ala 4F-Ph 3F,4Cl-Ph 40 52
33 α-Me-Ala 4F-Ph 2F,4F-Ph 110 90
34 α-Me-Ala 4F-Ph 3F,5F-Ph 220 244
a

Values are the mean of at least two experiments.