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Table 2 Summary of medicinal chemistry studies

From: Malaria in South America: a drug discovery perspective

Compound Authors Target Chemical class Lowest IC50(strain)
6 Sperandeo and Brun [[66]] - Pyrazolylnaphthoquinones, 5-aminoisoxazole 0.11 μg/mL (K1)
7 Silva et al.[67] - 1,4-naphthoquinones 0.03 μM (FcB1)
8 Charris et al.[68] β-haematin Thieno(2,3-b)quinoline 74.42%1
9 Cunico et al.[69] Aspartyl protease Hydroxyethylpiperazines 4.6 μM (3D7)
10 Cunico et al.[70] Aspartyl protease Hydroxyethyylpiperazines 5.1 μg/mL (W2)
11 Gnoatto et al.[71] β-haematin Piperazine, 3-acetylursolic acid 0.08 μM (FcB1)
12 de Sá et al.[72]   Betulinic acid 5.99 μM (W2)
13 Pinheiro et al.[73] - Sesquiterpenes 0.05 ng/mL (P. falciparum mefloquine resistant)
14 Barbosa et al.[74] - Ozonides 13.6 μg/mL
15 Oliveira et al.[75] Cysteine proteases Semicarbazone, Thiosemicarbazone 7.2 μM (W2)
16 Camacho et al.[76] β-haematin Benzimidazole-5-carbohydrazides 8.43 μM
17 Corrales et al.[77] Hypoxanthine-guanine phosphoribosyltransferase 6-thiopurine Steroids 82%1
18 Barazarte et al.[78] β-haematin Pyrazolo and pyrimido benzothiazine dioxide 92.32%2
19 Barazarte et al.[79] β-haematin Benzothiazines 78.17%2
20 Vellasco Junior et al.[80] Aspartyl protease Thioetherhydroxyethyl, Sulfonamides 15 μM (W2)
21 Dominguez et al.[81] β-haematin Chlorovinyl sulfones 0.025 μM (W2)
22 Dominguez et al.[82] β-haematin Sulfonamide chalcones 0.48 μM (W2)
23 León et al.[83] Glucose metabolism β-haematin Sulfonylureas 1.2 μM (W2)
24 Arancibia et al.[84] β-haematin Rhenium bioorganometalics, Aminoquinoline 0.048 μM (3D7)
25 Rojas Ruiz et al.[85] β-haematin Aminoquinolines, thiazolidinone 0.25 μM (3D7)
26 Charris et al.[86] β-haematin E-2-quinolinylbenzo-cycloalcanones 90%3
27 Vashist et al.[87] β-haematin Quinolone, 6-thiopurine inactive
28 de Souza et al.[88] β-haematin 4-aminoquinolines, platinum (II) complexes 84 %4
29 Cunico et al.[89] β-haematin 4-aminoquinolines 1.39 μg/mL (W2)
30 Rodrigues et al.[90] β-haematin Quinoline Active
31 Domínguez et al.[91] Cysteine protease falcipain Quinolinyl chalcones 19 μM (FcB1)
32 Ferrer et al.[92] β-haematin Chloroquinolines 94.93%3
33 Navarro et al.[93] β-haematin Gold-chloroquine complexes 5
34 Domínguez et al.[94] Cysteine protease β-haematin Phenylurenyl chalcones 1.76 μM
35 de Andrade-Neto et al.[95] - Naphthoquinones, Phenazines 1.67 μM (W2)
36 Hilário et al.[96] - 3-alkylpyridines alkaloids <3.38 μM (W2)
37 Rodrigues et al.[97] β-haematin Bisquinoline 56.76 %2
  1. 1 Percentage of inhibition of parasite growth (P. berghei in mice) at day 9 (dose: 10 mg/kg).
  2. 2 Inhibition of globin proteolysis (IGP) expressed as percentage.
  3. 3 Inhibition of β-haematin synthesis (IβHS) expressed as percentage.
  4. 4 Inhibition of parasite multiplication on days (dose: 25 mg/kg).
  5. 5 Activity expressed as IC50(CQDP)/IC50(complex).