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. 2009 Dec 15;19(24):6970–6974. doi: 10.1016/j.bmcl.2009.10.050

Table 4.

Piperidyl benzamides SAR: bicyclic amine modifications

graphic file with name fx31.jpg

Compds R1 R2 P. falciparum 3D7 strain EC50, μMa P. falciparum W2 strain EC50, μMa
8 Cl graphic file with name fx32.gif 0.134 0.888
30 Cl graphic file with name fx33.gif 0.082 0.296
31 CF3 graphic file with name fx34.gif 0.149 0.299
32 Cl graphic file with name fx35.gif 0.140 0.323
33 CF3 graphic file with name fx36.gif 1.49 1.41
34 CF3 graphic file with name fx37.gif 0.058 0.211
35 CF3 graphic file with name fx38.gif 0.175 0.635
a

Values are means of two experiments. Each assay plate has mefloquine, sulfadoxine and artimesinin as internal standards. The EC50 values for standard compounds match the literature values.