parasitemia

Piperaquine is a bis-quinoline antimalarial compound, a companion compound to artemisinin.Piperaquine is a component of Eurartesim, which is commonly used in the study of malaria infections.

Fosravuconazole L-lysine ethanolate (BMS-379224 L-lysine ethanolate) is a broad-spectrum antifungal agent approved in Japan for treating onychomycosis, a fungal nail infection. It is a prodrug converted into ravuconazole.

Moxipraquine is a novel 8-aminoquinolone compound with anti-infective activity against Trypanosoma cruzi. Moxipraquine effectively inhibited parasitemia but did not eradicate infections in mice or guinea pigs. Moxipraquine was effective against experimental infections of Leishmania major, Lactobacillus mexicanus, and Lactobacillus brasiliensis, but was Ineffective.

Insecticidal agent 24 is an orally active pyridinyl spiroindoline lead compound. It demonstrates antimalarial activity with Pf NF54IC50 of 0.08 μM. Insecticidal agent 24 also inhibits hERG activity with an IC50 of 6.5 μM. In a humanized immunodeficient NSG mouse model of malaria infection, it effectively reduces parasitemia.

DMU759 is a lysyl-tRNA synthetase 1 (KRS1) inhibitor. It exhibits potent anti-kinetoplastid activity against Trypanosoma cruzi, Trypanosoma brucei, and Leishmania donovani. In mouse models of acute Chagas disease, DMU759 significantly reduces parasitemia. DMU759 is applicable for research on parasitic infections, including Chagas disease.

PI4K-IN-3 (Compound 27) is an orally effective PI4K inhibitor with an IC50 of 1.9 nM for Plasmodium vivax PI4K. It does not inhibit the hERG channel and is non-cytotoxic to mammalian cells. This compound shows notable selectivity for human MINK1 and MAP4K4 kinases but has lower selectivity for human PI3Kα and PI4Kβ. PI4K-IN-3 exhibits potent antimalarial activity, significantly reducing parasitemia in NSG mouse models infected with Plasmodium falciparum.

Violacein is a bacterial metabolite originally isolated from C. violaceum that has antibacterial and antiprotozoal activities.[1] [2] It is produced by C. violaceum as a purple pigment in response to N-hexanoyl homoserine lactone , a property that has been modified to create a strain of C. violaceum used in detecting quorum-sensing molecules.[3] Violacein is active against Gram-positive bacteria, including B. subtilis and S. aureus (MICs = 0.8 and 1.6 µM, respectively). It is also active against P. falciparum, including chloroquine-susceptible and -resistant strains (IC50s = 0.85 and 0.63 µM, respectively).[2] It reduces parasitemia in a mouse model of nonlethal P. chabaudi chabaudi infection when administered at a dose of 7.5 mg/kg and increases survival in a mouse model of lethal P. chabaudi chabaudi infection. Violacein permeabilizes the cytoplasmic membrane of bacterial cells but does not affect the cell wall.[1]

Purfalcamine is an orally active, selective Plasmodium falciparum calcium-dependent protein kinase 1 (PfCDPK1) inhibitor with an IC50 of 17 nM and an EC50 of 230 nM, exhibiting antimalarial activity by inducing developmental arrest of malaria parasites at the schizont stage[1][2].

JMI-105 has the potential as an antimalarial agent. JMI-105 is a potent inhibitor of Plasmodium falciparum falcipain-2 protease (PfFP-2) that inhibits the P. falciparum strains CQ S (3D7) and CQ R (RKL-9) growth with IC 50 values of 8.8 μM and 14.3 μM. In a murine model with P. berghei ANKA infection, JMI-105 significantly decreases parasitemia and prolonged host survival [1].

SJ000025081 is a dihydropyridine and can be used as an antimalarial agent. In a mouse malaria model, SJ000025081 significantly inhibited parasitemia in P. yoelii infection.

FTI-2628 is a novel inhibitor of protein farnesyltransferase (FT), inhibiting the growth of P. falciparum in red blood cells and suppressing parasitemia.

Antimalarial agent 26, a derivative of 1,4-naphthoquinones, demonstrates antimalarial properties through oral administration. It exhibits cytotoxic effects on P. falciparum while maintaining selectivity against mammalian cell lines and effectively inhibits P. berghei-induced parasitemia in vivo [1].

Antimalarial agent 25, a derivative of 1,4-naphthoquinones, demonstrates oral activity and is effective against malaria. It exhibits cytotoxic properties specifically targeting P. falciparum and effectively inhibits parasitemia induced by P. burghei in vivo [1].