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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