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. 2018 Mar 27;6:88. doi: 10.3389/fchem.2018.00088

Table 2.

Efficiency of compounds for peripheral targeting.

Target Parasite species Compound name Effect on protein Effect on parasite Cell stage in vitro Effect in vivo Host species Reference
HT Plasmodium spp. Inline graphic
TCMDC-125163
IC50
39 nM
IC50
1.24 μM
Trophozoites Ortiz et al., 2015
Inline graphic
C3361
Ki
8.6–53 μM
IC50
15–16 μM
Trophozoites Joet et al., 2003; Blume et al., 2011
IC50
11 μM
Liver-stage Human Slavic et al., 2011
HT1 B. bovis Ki
4.1 μM
No inhibition at 100 μM Trophozoites de Muylder et al., 2011
GT1 T. gondii Ki
82 μM
No inhibition at 200 μM Tachyzoites Blume et al., 2011
FNT P. falciparum Inline graphic
MMV007839
IC50
0.02–0.17 μM
IC50
0.14 μM
Trophozoites Golldack et al., 2017; Hapuarachchi et al., 2017
Inline graphic
MMV000972
IC50
0.05–0.17 μM
IC50
1.70 μM
Trophozoites
PT0 T. brucei Inline graphic
UK5099
Inhibition at 250 μM Sanchez, 2013
PAT12 T.cruzi Inline graphic
Isotretinoin
IC50
0.13 μM
Epimastigotes Reigada et al., 2017
IC50
30.6 μM
Trypomastigotes
ENT1 Plasmodium spp. Inline graphic
ChemBridge 9001893 Inline graphic
ChemBridge 6946484
IC50
2.5–30 nM
IC50
3–55 μM
Trophozoites Frame et al., 2015b
ATP4 P. falciparum Inline graphic
Cipargamin
IC50
0.5–1.4 nM
Trophozoites Clearance with 3-day dosing, 30 mg per day Human Rottmann et al., 2010; Spillman and Kirk, 2015
Inline graphic
SJ733
IC50
30 μM
Trophozoites Spillman and Kirk, 2015
Calcium channels Leishmania spp. Trypanosoma spp. Inline graphic
1,4-dihydropyridines (e.g., Nifedipine)
−− IC50
2.6–181 μM
Promastigotes/Amastigotes Trypomastigotes −− −− Tempone et al., 2009 Reimão et al., 2010, 2011
A. castellanii Inline graphic
Amlodipine
Large inhibition at 1.2 μM Trophozoites Baig et al., 2013
L. infantum Inline graphic
Non-dihydropyridines (e.g., fendiline)
IC50
2–16 μM
Promastigotes Reimão et al., 2016
T. cruzi Epimastigotes Reimão et al., 2016
K1/K2 T. brucei Inline graphic
Fluticasone
IC50
0.7 μM
Schmidt et al., 2017