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Table 1 Summary of in vitro and in vivo PfA-M1 inhibitors properties

From: Selective inhibition of PfA-M1, over PfA-M17, by an amino-benzosuberone derivative blocks malaria parasites development in vitro and in vivo

  Structure Ki rPfA M1 (nM) Ki rPfA M17 (nM) IC50 in vitro (µM) In vitro strain In vivo model In vivo parasitaemia reduction (%) References
CHR-2863 1413.41 ± 123.74 75.96 ± 22.86 0.37 3D7 P. c. chabaudi/C57/BL6j 43% (25 mg/kg) [46]
0.376 K1
52% (50 mg/kg)
66% (100–50 mg/kg)
Bestatin 1673.00 ± 238.05 613 ± 201.33 5 3D7 P. c. chabaudi/8 weeks old C57/BL6j 34% at 100 mg/kg, twice a day [46, 47]
12–21 Dd2
25 ± 1.2 11–15 D10
8–14 3D7
Malarone NA NA P. c. chabaudi/C57/BL6j 100% at 14 mg/kg [46]
Chloroquine 10.1 ± 3.8 3D7 P. c. chabaudi/8 weeks old C57BL/6j 85% at 5 mg/kg [47]
138.0 ± 21.1 FcB1
Compound 4 79 13.2 ± 0.5 20–40 Dd2 P. c. chabaudi/8 weeks old C57BL/6j 92% at 100 mg/kg, twice a day [31, 47]
46–75 D10
24–62 3D7
T5 50 > 100 µM 11.2 ± 3.4 3D7 P. c. chabaudi/BALB/c 44 and 40% at 12 and 24 mg/kg/day this work
6.5 ± 2.4 FcB1
  1. NA data not available