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Table 2 Antiplasmodial activity of 1, 4-disubstituted piperidines on P. falciparum 3D7 and Dd2 strains

From: Structurally simple synthetic 1, 4-disubstituted piperidines with high selectivity for resistant Plasmodium falciparum

Compound code IC values (μg/mL)
3D7 Dd2
IC50 IC90 IC50 IC90
1 8.45 ± 2.11 17.85 ± 0.18 5.69 ± 2.38 27.59 ± 0.78
2 4.30 ± 3.75 17.61 ± 0.06 5.97 ± 0.02 24.86 ± 4.14
3 3.21 ± 0.21 17.9 ± 2.39 4.12 ± 1.28 32.38 ± 0.67
4 ND ND ND ND
5 10.02 ± 0.30 17.23 ± 0.97 14.51 ± 1.34 32.31 ± 4.17
6 13.63 ± 0.31 19.08 ± 2.46 12.75 ± 3.21 37.15 ± 0.53
7 4.00 ± 0.67 14.61 ± 1.52 a2.52 ± 0.77 17.71 ± 4.34
8 4.43 ± 0.32 13.89 ± 1.25 a1.30 ± 0.47 17.33 ± 3.27
9 1.53 ± 0.24 16.08 ± 2.13 1.67 ± 0.24 16.08 ± 2.13
10 13.54 ± 0.54 19.11 ± 0.02 13.98 ± 1.76 35.28 ± 2.02
11 2.51 ± 0.30 16.80 ± 0.88 a1.03 ± 0.124 27.82 ± 0.98
12 3.37 ± 0.82 15.74 ± 0.00 2.78 ± 0.09 10.2 ± 3.31
13 5.88 ± 2.49 8.94 ± 2.50 5.38 ± 0.69 25.93 ± 2.83
14 2.28 ± 0.64 11.31 ± 3.50 2.57 ± 1.64 16.21 ± 0.35
Art 0.045 0.039 ± 0.00 0.046 ± 0.00
QN 0.171 0.127
  1. 3D7 is a chloroquine-sensitive P. falciparum strain. -Not done, Art artemether, QN quinine. ND not determined due to low activity in the primary screen. Chemical classes of compounds:- carbonyls:16; alcohols: 712, and amines: 1314. aCompounds more active on chloroquine-resistant Dd2 than 3D7