Table 1 Inhibition of hemolysis exerted through wild-type PLY by pore-blocking agents PB-1 to PB-3 and derivatives (distinct samples n ≥ 3)

From: Targeted small molecule inhibitors blocking the cytolytic effects of pneumolysin and homologous toxins

Compound

Structure

IC50 [µM]a (95% CI)

PB-1

38 ± 6

PB-2

4.8 ± 0.8

PB-2.1

Inactive

PB-2.2

Inactiveb

PB-2.3

Inactive

PB-2.4

Inactive

PB-2.5

13 ± 1.7

PB-2.12

51 ± 1.6

PB-3

3.1 ± 0.5 (0.22 ± 0.09)c

  1. aIncubation with PLY for 10 min, for details see “Methods” section.
  2. bNo activity under standard conditions; prolonged incubation for 1.5 h yielded an IC50 value of 18 µM.
  3. cWith 2.5% human serum. For extended SAR with 46 further derivatives, see Supplementary Figs. 7, 8, and 14.
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