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. 2021 Sep 2;16(22):3396–3401. doi: 10.1002/cmdc.202100509

Table 2.

Activity of mono‐N‐aryl pentamidine analogues 3036 against kinetoplastid parasites.

Entry

Compound

T. b. brucei

T. congolense

L. mexicana

EC50 [μM; n=3]

RF

t‐test

EC50 [μM; n=3]

RF

t‐test

EC50 [μM; n=4]

WT

B48

WT

DA‐Res

1

30

1.10±0.07

1.31±0.02

1.19

0.042

2.94±0.10

3.26±0.01

1.11

0.037

12.7±0.7

2

31

0.91±0.02

0.86±0.02

0.94

0.10

n.d.

n.d.

2.12±0.07

3

32

0.65±0.03

0.37±0.006

0.57

0.0007

1.26±0.03

1.56±0.06

1.23

0.012

9.71±0.56

4

33

0.19±0.003

0.28±0.006

1.47

0.0002

0.64±0.02

0.75±0.003

1.23

0.0008

0.66±0.04

5

34

0.51±0.004

0.51±0.02

1.01

0.82

n.d.

n.d.

>20

6

35

1.09±0.01

0.82±0.01

0.75

0.0001

n.d.

n.d.

>20

7

36

3.04±0.02

2.98±0.04

0.98

0.23

6.69±0.11

9.29±0.17

1.39

0.0002

7.54±0.59

8

PMD

0.0024±0.0002

0.28±0.002

116

3.5×10−8

1.31±0.02

1.42±0.01

1.08

0.013

2.04±0.04

9

DA

0.082±0.006

0.89±0.05

10.8

0.0001

0.27±0.008

1.71±0.02

6.4

2×10−7

n.d.

WT=wild‐type, PMD=pentamidine, DA=diminazene aceturate, DA‐Res=diminazene‐resistant cell line, RF=resistance factor being the ratio of EC50 (resistant line) over EC50(WT). Statistical difference between WT and resistant pairs of cell lines was established using a Student unpaired two‐tailed t‐test.