Table 1 In vitro antitrypanosomal activity (IC50epi) of THD1-10 against epimastigote forms of the Trypanosoma cruzi, toxicity (CC50) to LLC-MK2 cells, and selectivity index (SI).

From: In vitro assays identified thiohydantoins with anti-trypanosomatid activity and molecular modelling studies indicated possible selective CYP51 inhibition

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R

IC50epi (µg/mL)

CC50 (µg/mL)

SI

THD1

H

12.8

493

38.6

THD2

CH3

44.1

541

12.3

THD3

CHCH3

19.9

421

21.2

THD4

Isopropyl

89.8

443

4.93

THD5

Isobutyl

18.8

516

27.5

THD6

(CH2)2SCH3

51.2

564

11.0

THD7

Pyrrolidine

77.5

459

5.91

THD8

Bn

62.1

368

5.92

THD9

p-OH-Bn

58.0

917

15.8

THD10

CH2-3-indole

153

107

0.69

BZN*

-

1.57

257

163

  1. In bold are the compounds with the most promising activity of the series. *BZN (benznidazole).
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