Table 1 Chemical structures of the quinoxaline derivatives (2a–2i, 3a–3i, and 4a–4d) and the corresponding in vitro inhibitory activities (IC50, μM) against the promastigote forms of Leishmania amazonensis11.

From: Quinoxalines against Leishmania amazonensis: SAR study, proposition of a new derivative, QSAR prediction, synthesis, and biological evaluation

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#

R1

R2

R3

R4

IC50 (µM)

pIC50 (M)

2a

H

OMe

NMe2

SMe

42.8

4.37

2b

H

OMe

NH(n-Bu)

SMe

35.2

4.45

2c

H

OMe

NH(cyclohexyl)

SMe

29.8

4.53

2d

OMe

H

NH(isopentyl)

SMe

27.1

4.57

2e

Br

H

NH(n-Bu)

SMe

25.2

4.60

2f

H

OMe

NH(isobutyl)

SMe

27.6

4.56

2g

Cl

H

NH(n-Bu)

SMe

24.4

4.61

2h

OMe

H

NH(isobutyl)

SMe

26.9

4.57

2i

OMe

H

NH(n-Bu)

SMe

30.2

4.52

3a

H

OMe

NH(n-Bu)

SO2Me

2.5

5.60

3b

H

OMe

NH(cyclohexyl)

SO2Me

2.9

5.54

3c

Br

H

NH(n-Bu)

SO2Me

1.6

5.80

3d

H

OMe

NH(isobutyl)

SO2Me

2.6

5.59

3e

Cl

H

NH(n-Bu)

SO2Me

1.4

5.85

3f

Cl

H

NH(cyclohexyl)

SO2Me

2.2

5.66

3g

H

H

NH(n-Bu)

SO2Me

2.9

5.54

3h

Br

H

NH(EtOH)

SO2Me

0.8

6.10

3i

Br

H

Cl

SO2Me

0.2

6.70

4a

Cl

Cl

Ph

Ph

5.3

5.28

4b

H

H

4-OMe-Ph

4-OMe-Ph

30.0

4.52

4c

H

H

4-Me-Ph

Ph

8.9

5.05

4d

H

H

4-OMe-Ph

Ph

12.8

4.89

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