Table 1 Antileishmanial and cytotoxic activities of compounds 46, 83, 92, 99 and 100.

From: Biochemical analysis of leishmanial and human GDP-Mannose Pyrophosphorylases and selection of inhibitors as new leads

Compounds

IC50 (µM) ± SD

 

Selectivity index (CC50/IC50)

L. donovani

L. mexicana

Cytotoxicity CC50 (µM) ± SD

L. donovani

L. mexicana

axenic amastigotes

infected RAW.264.7 macrophages

infected BMDMb

axenic amastigotes

infected RAW.264.7 macrophages

infected BMDMb

RAW264.7 macrophages

BMDMb

RAW264.7 macrophages

BMDMb

RAW264.7 macrophages

BMDMb

46

>100

>100

12.54 ± 0.93

7.69 ± 0.56

11.72 ± 1.13

15.71 ± 3.48

>100

13.10 ± 1.67

—

1.0

>8.5

0.8

83

>100

51.88 ± 7.49

27.14 ± 2.04

30.64 ± 3.29

45.41 ± 6.21

25.92 ± 5.37

>100

23.76 ± 1.98

>1.9

0.9

>2.2

0.9

92

>100

41.60 ± 13.99

82.45 ± 7.61

43.15 ± 3.42

8.25 ± 1.07

79.29 ± 9.76

>100

77.54 ± 5.34

>2.4

0.9

>12.1

1.0

99

1.06 ± 0.10

0.63 ± 0.14

1.06 ± 0.41

>100

1.49 ± 0.26

8.59 ± 2.44

1.53 ± 0.17

>100

2.4

>94.3

1.0

>11.6

100

30.68 ± 6.62

19.52 ± 4.53

12.18 ± 4.74

49.25 ± 0.26

27.52 ± 2.23

12.05 ± 1.27

62.06 ± 7.39

51.36 ± 3.45

3.2

4.2

2.3

4.3

Miltefosinea

2.08 ± 0.24

1.83 ± 0.22

0.83 ± 0.12

23.74 ± 2.81

52.62 ± 4.98

51.39 ± 5.34

>25

>25

13.7

>30.1

>0.5

>0.5

  1. The results expressed correspond to the mean of three independent experiments (±SD).
  2. (a) Miltefosine: reference compound.
  3. (b) BMDM: Bone Marrow Derived Macrophages.
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