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Table 3 Effects of amide 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

MC24A24

5.276

28.56

0.61 ± 0.09

11.52 ± 1.38

MC24A4I

5.746

11.82

1.06 ± 0.15

3.25 ± 0.62

MC23A24

5.276

10.00

0.26 ± 0.04

1.42 ± 0.14

MC08A27

5.498

13.50

0.66 ± 0.11

13.01 ± 1.49

BG31A02

4.721

1.82

0.50 ± 0.08

52.17 ± 3.43

BG21A11

3.203

4.44

NIb

61.07 ± 7.54

HH27A43

4.101

4.40

1.49 ± 0.24

16.09 ± 3.94

HH29A43

1.610

4.40

NI

20.49 ± 1.87

HH25A43

1.140

4.72

NI

49.70 ± 11.32

  1. a Data reflect the mean Ki ± SD (n = 3).
  2. b No inhibition.