malaria parasite

Dehydroemetine is an effective antigenic insecticide, which is a synthetic analogue of Emetine dihydrochloride. It can be used to prevent and treat amoeba infections and diseases. It has the effect of treating leishmania infection with skin damage and resistance to metronidazole amoebiosis.

Chloroquine is a Toll-like receptor inhibitor that inhibits autophagy. Chloroquine has anti-malarial and anti-inflammatory activity and is widely used in the treatment of malaria and rheumatoid arthritis. Chloroquine also has anti-SARS-CoV-2 (COVID-19) activity and anti-HIV-1 activity.

Pyronaridine is an orally active, mannitol-containing anti-malarial compound that acts by interfering with the replication of the malaria parasite (Plasmodium) within red blood cells. Pyronaridine is often used in combination with other drugs to treat malaria and has infective activity against P. falciparum and Echinococcus granulosus.

Chloroquine phosphate (Aralen phosphate) is an aminoquinoline antimalarial and also is widely used as an autophagy inhibitor. Chloroquine also is an inhibitor of toll-like receptors (TLRs).

Quinine is a natural cinchona alkaloid that has been used for centuries in the prevention and therapy of malaria. Quinine is also used for idiopathic muscle cramps. Quinine therapy has been associated with rare instances of hypersensitivity reactions which can be accompanied by hepatitis and mild jaundice.

Primaquine diphosphate is the phosphate salt form of primaquine, a synthetic, 8-aminoquinoline derivative with antimalarial properties. Although its mechanism of action is unclear, primaquine bind to and alter the properties of protozoal DNA. This agent eliminates tissue (exo-erythrocytic) malarial infection, preventing the development of the erythrocytic forms of the parasite which are responsible for relapses in Plasmodium vivax and ovale malaria. Primaquine is active against late hepatic stages (hypnozoites, schizonts).

Atovaquone (Atavaquone) is a hydroxynaphthoquinone that has antimicrobial activity and is being used in antimalarial protocols.

Fmoc-N-Me-Phe-OH (Fmoc-N-methyl-L-phenylalanine) is a Malaria Parasite inhibitor.

Quinidine is a stereoisomer of the antimalarial agent quinine and a class Ia antiarrhythmic agent. for the treatment of abnormal heart rhythms and also malaria.

Nerolidol acetate is a natural sesquiterpene with anti-cancer, anti-inflammatory, antibacterial and anti-insect activities. Nerolidol acetate can inhibit parasite activity and inhibit schistosomiasis, nematodes, malaria, etc. Nerolidol acetate protects cells from oxidative damage to lipids, proteins and DNA, and has a protective effect on mouse hippocampal nerve cells.

DDD01035881 is a novel and highly potent anti-malarial drug that blocks parasite-to-mosquito transmission with nanomolar activity by targeting the Plasmodium vesicle membrane protein Pfs16 and blocking the formation of male gametes in the life cycle of the malaria parasite.

PfDHODH-IN-2 is a dihydrothiophenone derivative, is a potent Plasmodium falciparum dihydroorotate dehydrogenase (PfDHODH, IC50 : 1.11 μM) inhibitor . It is used an antimalarial agent and can be used for the research of malaria

Chloroquine is a medication preventing and treating malaria in areas where malaria is known to be sensitive to its effects. It is also sometimes used for amebiasis that is occurring outside the intestines, rheumatoid arthritis, and lupus erythematosus. Ch

L-Canaline, a nonprotein amino acid found in many leguminous plants, exhibits potent anticancer and antiproliferative effects. It effectively inhibits the growth of the malaria parasite Plasmodium falciparum with an IC50 of 297 nM. Additionally, L-Canaline acts as a cytotoxic metabolite produced from L-canavanine through arginase catalysis and serves as a potent and irreversible inhibitor of ornithine aminotransferase.

SIBA (5'-Deoxy-5'-isobutylthioadenosine) is a synthetic analogue of SAH, acts as an inhibitor of S-adenosylmethionine-mediated transmethylation. SIBA can interfere with a variety of enzymatic activities in vitro, such as SAH hydrolase, methylthioadenosine phosphorylase and cAMP phosphodiesterase. SIBA reversibly blocks the multiplication of herpes simplex type 1 virus (HSV)

SID 26681509 is a selective, reversible and competitive human cathepsin L inhibitor (IC50 of 56 nM).

Nanaomycin A, a quinone antibiotics, reactivates silenced tumor suppressor genes in human cancer cells. Nanaomycin A is a selective inhibitor of DNMT3B (IC50 = 500 nM).

Antiproliferative agent-56 (Compound 31) is an antimalarial agent that inhibits the Pf3D7 strain of the malaria parasite Plasmodium falciparum with an IC50 of >12.5 (48h) and 0.03 μM (98h), displaying slow-acting characteristics.

DHFR-IN-20 (Compound LA1) is an inhibitor of dihydrofolate reductase (DHFR) targeting the malignant strains of the malaria parasite. It exhibits inhibition constants (Kis) of 0.16 nM, 0.30 nM, and 6.6 nM for PfDHFR-WT, PfDHFR-QM, and HsDHFR, respectively. Additionally, DHFR-IN-20 demonstrates antimalarial activity, with IC50 values of 1.4 nM against parasites carrying the wild-type (TM4 8.2) PfDHFR enzyme and 1.6 μM against those with the quadruple mutation (V1 S)PfDHFR.

MED6-189, an analog of kalihinol, disrupts the apicoplast functions and vesicular transport in the malignant malaria parasite (P. falciparum, IC50 < 50 nM). The compound specifically targets the apicoplast, which is a non-photosynthetic plastid essential for isoprenoid synthesis, found in most apicomplexan parasites.

PfCLK3-IN-1 (Compound 4) serves as a covalent inhibitor of the malaria parasite CLK3 (Pf CLK3) under alkaline conditions, with a pEC50 of 7.1. It inhibits the maturation of gametocytes during the sexual stage of the parasite, thereby hindering transmission. Additionally, PfCLK3-IN-1 effectively suppresses the Dd2-B2 clone of the malaria parasite, exhibiting an IC50 of 239.5 nM.

SPB07935 inhibits plasmepsin II in the malaria-causing parasite Plasmodium falciparum and serves as an antimalarial agent. It affects the life cycle of P. falciparum, hindering the growth of the parasite's FcB1 and 3D7 strains, with IC50 values of 8 μM and 4.7 μM, respectively.

DS-103 is an HDAC inhibitor that targets HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8 with IC50 values of 0.029, 0.123, 0.022, 0.367, and 9.26 μM, respectively. It also inhibits the malignant malaria parasite [Plasmodium falciparum 3D7] with an IC50 of 5.08 μM. In A2780 and Cal27 cells, DS-103 exhibits cytotoxicity with IC50 values of 1.48 μM and 1.47 μM, respectively, and reverses cisplatin resistance in these cells with IC50 values of 4.62 μM and 2.23 μM. DS-103 acts synergistically with cisplatin, enhancing apoptosis induced by cisplatin.

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].