Table 2 IC50 (µM) values of various syntheses of thiosemicarbazone-derived series against L. tropica and L. major amastigotes and promastigotes forms, cytotoxicity evaluation (CC50) on J774A.1 cell line, and SI calculated on amastigote forms. Data are described as the mean ± sd (n = 3).

From: Synthesis of thiosemicarbazone Schiff base derivatives as anti-leishmanial agents and molecular dynamics simulations insights

Compound

IC50 (µM)

CC50 (µM)

(J774 A.1 cell line)

SI

(CC50/IC50 of amastigotes)

IC50 (µM) L. major

(MRHO/IR/75/ER)

IC50 (µM) L. tropica

(MHOM/IR/02/Mash10)

L. major

(MRHO/IR/75/ER)

L. tropica

(MHOM/IR/89/ARA2)

Promastigotes

P-value

Vs. AmB

Amastigotes

P-value

Vs. GLU

Promastigotes

P-value

Amastigotes

P-value

5a

54.3 ± 3.9

p > 0.05

60 ± 4.1

P < 0.0001

258 ± 13.8

p > 0.05

453.9 ± 8.14

p < 0.05

1654 ± 10

27.5

3.6

5b

38.3 ± 2.6

p > 0.05

111.8 ± 6

P < 0.001

199.8 ± 9.6

p > 0.05

248.3 ± 7.39

P < 0.01

1144 ± 10

10.2

4.6

5c

938 ± 22.1

p > 0.05

1109 ± 11

p > 0.05

1049.7 ± 22.7

p > 0.05

451.7 ± 9.5

P < 0.01

> 4825

-

-

5d

346 ± 9.7

p > 0.05

319.2 ± 8

p > 0.05

441.3 ± 8.9

p > 0.05

761.6 ± 9.57

p > 0.05

2373 ± 11.4

7.4

3.1

5e

65.3 ± 14.2

p > 0.05

31.8 ± 3.8

P < 0.0001

92.3 ± 10.9

p > 0.05

24.5 ± 5.77

P < 0.001

847 ± 10

26.6

34.6

5f

159.7 ± 11.4

p > 0.05

177.4 ± 5.8

P < 0.01

240 ± 15.8

p > 0.05

257.8 ± 6.76

P < 0.01

2639.6 ± 10.6

14.9

10.2

5g

26.7 ± 1.2

p > 0.05

18.8 ± 5.8

P < 0.0001

101.5 ± 9.7

p > 0.05

22.7 ± 3.06

P < 0.001

733.2 ± 9.2

39

32.2

5h

> 4450

p > 0.05

2400 ± 12.2

p > 0.05

> 4450

-

> 4450

-

3392 ± 9.2

1.4

-

5i

88.8 ± 5.3

p > 0.05

76.4 ± 2.1

P < 0.0001

192.6 ± 8.4

p > 0.05

185.9 ± 4.95

P < 0.01

1483 ± 10.5

19.4

7.8

5j

433.2 ± 7.6

p > 0.05

424.3 ± 4

P > 0.05

1236.2 ± 9.2

p > 0.05

1143.9 ± 10.3

p > 0.05

2800 ± 10.4

6.6

2.4

5k

1200.7 ± 8.8

p > 0.05

845 ± 3.8

p > 0.05

865.1 ± 8.4

p > 0.05

774.6 ± 5.3

p > 0.05

> 1000

-

-

5l

346 ± 7.1

p > 0.05

680.5 ± 4.4

p > 0.05

389.5 ± 6.2

p > 0.05

331.4 ± 8.6

p > 0.05

1062 ± 8.3

1.5

3.2

5m

1000 ± 9.8

p > 0.05

891.6 ± 7.6

p > 0.05

642.3 ± 7.7

p > 0.05

349.6 ± 12.2

p > 0.05

1332 ± 9.1

1.5

3.81

5n

891 ± 7.5

p > 0.05

626.9 ± 8.3

p > 0.05

550.8 ± 6.6

p > 0.05

474.6 ± 11.3

p > 0.05

2853 ± 8.6

4.5

6

5o

1079 ± 7.9

p > 0.05

886 ± 4.7

p > 0.05

> 1000

-

> 1000

-

1806 ± 8.5

2

-

5p

31.2 ± 3.3

p > 0.05

12.77 ± 1.8

P < 0.0001

313.9 ± 6.9

p > 0.05

200.8 ± 5.1

P < 0.01

1218 ± 8.2

95.4

6.1

GLU

888 ± 11

NR

243 ± 6

NR

1051 ± 9

NR

300.5 ± 9.7

NR

2431 ± 9.5

10

8.09

AmB

9.6 ± 1

NR

17.5 ± 1.1

NR

17.9 ± 2.1

NR

27.9 ± 2.9

NR

1695 ± 2.8

96.9

61

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