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 |