|
Chemical compound Structure | Chemical family | Target | Mode of action | IC50 (M) | Ki (nM) | Antimalarial effect | Origin | References |
|
| Spergualin derivate | Apicoplast protein synthesis | Suggested inhibition of chaperone-transit peptide interactions
| 0.15 | | Delayed death | Bacillus laterosporus | [7–9] |
| Tetracycline derivate | Apicoplast protein synthesis | Binding to microbial ribosomes and blocking the attachment of charged aminoacyl-tRNA | 10 | | Delayed death | Streptomyces spp
| [10, 11] |
| Phosphonic acid derivative | Apicoplast Isoprenoid biosynthesis | Inhibits specifically the DOXP reductoisomerase (DXR or Isp C) | 0.35 | | Immediate | Streptomyces lavendulae | [12–14] |
| Dipeptide | Aminopeptidase for example, PfM17LAP | Chelating of metal binding centres | 8–21 | 25 | | Streptomyces olivoreticuli | [15–17] |
| Phosphinate dipeptide analogue | Aminopeptidase for example, PfM17LAP
| Proposed chelation of active site metal ions | 20–75 | 13 | | Synthetic | [18, 19] |
| Phosphinate dipeptide analogue | Aminopeptidase for example, PfM17LAP | Proposed chelation of active site metal ions | 13–62 | 10 | | Synthetic | [18, 19] |
| Hexapeptide | PM I–IV | No direct effect on haemoglobin degradation | 4 | PMI: 0.4 PMII: 0.03 PMIII: 0.1 PMIV: 0.3 | | Actinomyces | [20, 21] |
| Peptidomimetic | PM II | Mimic Phe-Leu found in haemoglobin alpha chain | 0.04 | 0.5 | | Synthetic | [22–24] |
| Peptidomimetic | PM I, II, IV | | n.d. | I: 21 ii: 25 IV: 46 | Expanded lifespan of mice (up to 171%) | Synthetic | [25] |
| Peptidomimetic
| PMII | | 0.1 | | Expanded lifespan of mice (up to 161%) | Synthetic | [25] |
| Aryl amino alcohol | Not precisely known, but effective against plasmepsin I–III | | 0.001–0.006 | | | Classical antimalarial drug with unknown mode of action, developed as synthetic quinine analogue | [25–27] |
| Peptidomimetic | PMV | Inhibits the PMV cleavage of a PEXEL peptide | 70 | | | HIV protease inhibitor | [25] |
| Peptidomimetic | PMV | Inhibits the PMV cleavage of a PEXEL peptide | n.d. | | | HIV protease inhibitor | [25] |
| Peptidomimetic | PMV | Inhibits the PMV cleavage of a PEXEL peptide | 15 | | | HIV protease inhibitor | [25] |
| Peptidomimetic | PMV | Inhibits the PMV cleavage of a PEXEL peptide | n.d. | | | HIV protease inhibitor | [25] |
|