antimalarial

Mepacrine (Erion) is an acridine derivative formerly widely used as an antimalarial. It is used in cell biological experiments as an inhibitor of phospholipase A2.

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.

Pyrimethamine (Pirimecidan) is a competitive inhibitor of dihydrofolate reductase (DHFR), used as an antimalarial drug.

Mefloquine hydrochloride (Mefloquin hydrochloride) is a quinoline derivative used for the prevention and therapy of P. falciparum malaria.

Hexyl gallate (Gallic acid hexyl ester), an alkyl ester derivative of gallic acid, exhibits potent antimalarial activity against Plasmodium falciparum (IC50: 0.11 mM).

Lycorine (Narcissine) inhibits protein synthesis and may inhibit ascorbic acid biosynthesis, although studies on the latter are controversial and inconclusive.

Sulfadiazine sodium (Sulfadiazin-natrium) is a sodium salt form of sulfadiazine, an intermediate-acting bacteriostatic, synthetic sulfanilamide derivative.

Ferroquine (Ferrochloroquine) is a ferrocenyl analogue of Chloroquine with antimalarial activity. Ferroquine induces oxidative stress and the subsequent destruction of the membrane, resulting in parasiticidal effect on Plasmodium.

Amodiaquine dihydrochloride dihydrate (Amodiaquine hydrochloride) is the hydrochloride salt of amodiaquine, an orally active 4-aminoquinoline derivative with antimalarial and anti-inflammatory properties.

Mefloquine (Ro 215998), a quinoline antimalarial agent, is an anti-SARS-CoV-2 entry inhibitor. Mefloquine is also a K+ channel (KvQT1/minK) antagonist with an IC50 of ~1 μM. Mefloquine can be used for malaria, systemic lupus erythematosus, and cancer research.

Cletoquine is a major active metabolite of Hydroxychloroquine. Cletoquine has the ability to against the chikungunya virus (CHIKV). Cletoquine has antimalarial effects and has the potential for autoimmune disease treatment.

Tafenoquine Succinate (WR 238605 (Succinate)) is an 8-aminoquinoline. and is an agent of anti-malarial prophylactic.

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).

Ganaplacide phosphate exerts multi-stage antimalarial activity against Plasmodium symptomatic asexual blood-stage infections, and is able to prevent transmission and block infection in animal models.

Ethylhydrocupreine hydrochloride (Optochin hydrochloride) is a derivative of quinine with antimicrobial activity against Streptococcus pneumoniae and antimalarial activity with an IC50 of 25.75 nM against Plasmodium falciparum. It is also an agonist of Gallus gallus2 receptors (ggTas2r1, ggTas2r2, and ggTas2r7).

Proguanil hydrochloride (Chloroquanil) is a biguanide compound which metabolizes in the body to form cycloguanil, an anti-malaria agent.Upon hydrolysis, Proguanil hydrochloride is converted to its active cyclic triazine metabolite, cycloguanil, by a cytochrome P450 dependent reaction. Cycloguanil selectively inhibits the bifunctional dihydrofolate reductase-thymidylate synthase of plasmodium parasite, thereby disrupting deoxythymidylate synthesis and ultimately blocking DNA and protein synthesis in the parasite.

ELQ-300 is bioavailable antimalarial agent, acts as an inhibitor of the reductive (Qi) site of the cytochrome bc1 complex (cyt bc1)

1. Tuberostemonine (Tuberstemonine) exhibits relatively higher intestinal permeabilities. 2. Tuberostemonine acts in part as an open-channel blocker at the crayfish neuromuscular junction.

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.

Piperaquine tetraphosphate tetrahydrate is a potent anti-parasites agent.

Amodiaquine is a synthetic aminoquinoline, used to treat malaria.

INE963 demonstrates potent cellular activity against Pf 3D7 (EC50 = 6 nM) and achieves artemisinin-like kill kinetics in vitro with a parasite clearance time of <24 h. INE963 is also potent against P. falciparum and P. vivax clinical isolates from Brazil and Uganda with EC50's ranging from 0.01 to 7.0 nM

Febrifugine is an effective coccidiostat, possesses schizonticide props; it and its derivatives shows high degree of antimalarial activity but use limited by toxicity .

Febrifugine dihydrochloride (Propyldazine hydrochloride) is a biochemical with therapeutic activity regarding malaria, cancer, fibrosis and inflammatory diseases.