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Table 2 Effects of hydrazide derivatives on cultured T. b. brucei , purified trypanopain-Tb, and sheep cathepsin L

From: Chalcone, Acyl Hydrazide, and Related Amides Kill Cultured Trypanosoma brucei brucei

Compound

A

B

CLogP

T. b. brucei IC50 (µM)

Trypanopain Ki (µM)a

Cathepsin L Ki (µM)a

ZLIV44A

3.317

0.72

1.31 ± 0.20

9.48 ± 0.52

ZLIII43A

4.226

1.53

0.027 ± 0.002

1.49 ± 0.17

ZLIII115A

5.755

1.01

0.34 ± 0.04

0.90 ± 0.14

MC357

4.296

0.42

0.64 ± 0.08

1.07 ± 0.14

TF-1-58

2.215

1.44

1.20 ± 0.01

6.47 ± 1.18

TF-1-52

3.865

0.58

1.12 ± 0.24

1.59 ± 0.31

TF-1-54

4.255

2.34

3.45 ± 0.27

3.18 ± 0.48

TF-1-56

6.523

1.66

0.22 ± 0.06

1.90 ± 0.10

TF-1-51

4.273

1.55

4.47 ± 0.64

1.52 ± 0.28

TF-1-59

4.063

2.14

1.38 ± 0.14

3.81 ± 0.59

TF-1-53

4.376

2.70

2.74 ± 0.44

3.39 ± 0.31

TF-1-55

5.070

1.91

4.06 ± 0.66

2.32 ± 0.16

TF-1-60

4.632

1.02

0.39 ± 0.12

1.35 ± 0.21

  1. a Data reflect the mean Ki ± SD (n = 3).