malaria

Antimalarial agent 13 (N2-(3-chlorophenyl)-N4-(furan-2-ylmethyl)quinazoline-2,4-diamine) is a potent antimalarial agent.

Antimalarial agent 30 has anti-Plasmodium berghei liver stage parasite activity and antimalarial activity for the study of malarial infections.

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.

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).

Hydroxychloroquine (2-[[4-[(7-Chloroquinolin-4-yl)amino]pentyl](ethyl)amino]ethanol) (HCQ) is an alkalinizing lysosomatropic drug that acts by inducing apoptosis of renal cancer cells in vitro and inhibiting TLR7/9. It is a medication used to prevent and treat malaria, and it's also being studied as an experimental treatment for COVID-19.

Sulfalene (SMP2), a long-acting sulfonamide antibiotic, is used for the therapy of chronic bronchitis, urinary tract infections, and malaria.

ZY-19489 is an antimalarial compound that is a potential single-dose cure for Plasmodium falciparum and Plasmodium vivax malaria. It has received orphan drug designation from the FDA.

Antimalarial agent 33 (compound 5g) exhibits antiplasmodial activity targeting both erythrocytic and hepatic stages of Plasmodium, with an effective concentration (EC50) of 1.1 μM against the K1 strain of P. falciparum. It demonstrates improved microsomal stability with a half-life (T1/2) of 29 minutes and displays no significant cytotoxicity against primary hepatocytes [1].

Antimalarial agent 1 is an effective antimalarial agent.

DSM421 (DSM-421) is a dihydrodehydrogenase inhibitor (DHODH) that is in preclinical development as a potential treatment option for malaria and has shown activity against field isolates of both P. falciparum and P. vivax.

ST7612AA1 is a novel potent and oral HDCA inhibitor that acts as an HIV-1 latency reactivator. ST7612AA1 showed significant antitumor activity at low concentrations in vitro and in vivo. ST7612AA1 has potential anticancer activity and can be used to study malaria.

2'-Hydroxy-3,4-dimethoxychalcone, a chalcone compound isolated from the roots of Sophora japonica, has antioxidant activity and inhibited the intracellular survival of Lactobacillus donovani Parasite EC.50 Values ranged between 0.39 and 0.41 μg/mL, which can be used in the study of diabetes, treatment of schistosomiasis, malaria and other infections.

Demethyldaphnoretin-7-O-glucoside is a natural product that is isolated from Daphne oleoides Schreber subsp. kurdica (DOK). In Turkish traditional medicine, the aerial parts of DOK have been used to treat malaria, rheumatism and for wound healing.

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.

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.

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.

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.

4-(2-Aminoethyl)amino-7-chloroquinoline (N1-(7-Chloroquinolin-4-yl)ethane-1,2-diamine) has potential anthelmintic and antitumor activity for the study of malaria.

Antimalarial agent 8 (Compound 7e) is a novel, orally active antimalarial agent that is effective against P. falciparum in vitro and effective orally in an in vivo mouse model of malaria (40 mg/kg).

Compound 24 (Compound 7), an in vitro antimalarial agent, demonstrates inhibitory activity against the Plasmodium falciparum W2 strain with an IC50 of 0.81 μM and exhibits a cytotoxicity threshold (CC50) exceeding 200 μM in HepG2 cells [1].

Antimalarial agent 28 (Compound 2i) acts as an antiplasmodial agent, exhibiting inhibition of P. berghei with IC50 values of 0.561 μM for the liver stage, 0.14 μM for early gametocytes, and 4.34 μM for the ring stages of P. falciparum [1].

Compound 29 (also known as Compound 16) is an antimalarial agent that demonstrates inhibition of the P. berghei liver stage parasite load, exhibiting an effective concentration (EC50) of 5.2 μM [1].

Antimalarial agent 15 is a parasite inhibitor that exhibits antimalarial effects and inhibits the growth of Plasmodium falciparum 3D7 with an IC50 value of 20 nM.

Antimalarial agent 9 is an effective antimalarial agent, a quinoline-imidazole derivative compound. antimalarial agent 9 showed significant in vitro antimalarial effects against CQ-susceptible strains (IC50-0.14 μM) and MDR strains (IC50-0.41 μM), with minimal cytotoxicity and high selectivity.

Antimalarial agent 12 is an effective antimalarial agent that inhibits the growth of Plasmodium falciparum strains Dd2 and 3D7 with EC50 values of 155 nM and 136 nM, respectively. antimalarial agent 12 has a MIC >250,000 nM against E. coli and also acts on Antimalarial agent 12 has a MIC of >250,000 nM against E. coli and also works on HEK-293 and hPHep cell lines with CC50 values of 10,000-50,000 nM.

Antimalarial agent 23, a benzimidazole-based compound, exhibits potent antimalarial activity, demonstrated by its low IC50 values of 0.08 μM for PfNF54 and 0.10 μM for PfK1, respectively. This compound effectively inhibits β-hematin formation, yet it does not directly interfere with the conversion of heme to hemozoin [1].

Antimalarial agent 17, functioning both as an antimalarial agent and a herbicide, inhibits photosystem II and demonstrates post-emergence herbicidal efficacy comparable to commercial herbicides [1].

Antimalarial agent 16 is a parasite inhibitor that exhibits antimalarial effects and inhibits the growth of Plasmodium falciparum with an IC50 value of 2.0 nM.

Antimalarial agent 11 (compound 1) is a potent antimalarial agent, a spirocyclic chromane. Antimalarial agent 11 is able to act on D6 (EC50: 1.48 μM) and ARC08-022 (EC50: 1.81 μM).

Antimalarial agent 14 (NSC-102533) is a bioactive chemical.

Antimalarial agent 7 is a potent and effective inhibitor of PfATP4. Antimalarial agent 7 has potential for the study of the human plasmodium falciparum.

Antimalarial agent 27 (compound 11a) potently inhibits P. falciparum with an IC50 of 0.37 μM and targets the parasite's 1-deoxy-D-xylulose-5-phosphate reductoisomerase (DXR) enzyme with an IC50 of 0.11 μM, indicating its mechanism of action [1].

Antimalarial agent 20, exhibiting potent efficacy with an IC50 value of 0.6 nM against the P. falciparum NF54 parasite strain within the NF54 albumax assay, serves as a significant antimalarial compound.

Antimalarial agent 10 (Compound 17b) is an amino alcohol-quinoline compound. Antimalarial agent 10 is also an antimalarial agent capable of acting on Pf3D7 (IC50: 14.9 nM) and PfW2 (IC50: 11 nM) with a selectivity index greater than 770 regardless of the cell line.

Antimalarial agent 3, an antimalarial agent, exhibits potent activity against Plasmodium with an IC50 of 0.035 μM. Furthermore, it demonstrates an exceptionally high selectivity index in relation to mammalian cells.

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].

Compound 31 (compound 7k) is an orally active inhibitor of Plasmodium falciparum aspartic protease, plasmepsin X (PMX), with antimalarial properties [1].

Antimalarial agent 2 is an orally active, novel antimalarial agent that exhibits rapid in vitro killing effects.

Antimalarial agent 18, a powerful antimalarial compound characterized by its electronic, highly lipophilic, and siderophoric properties, falls within the acyloxymethyl series, acting as a fosmidomycin surrogate. It effectively inhibits the non-mevalonate isoprenoid biosynthesis pathway by targeting the IspC enzyme. This compound demonstrates significant inhibitory activity against P. falciparum (IC50 = 50 nM) and A. baumanii (IC50 = 390 nM).

Antimalarial agent 19 (compound 6e) exhibits antimalarial activity against the blood stages of P. falciparum K1 and P. berghei, with EC50 values of 0.3 µM and 15.3 µM, respectively. It demonstrates good aqueous solubility, intestinal permeability, and microsomal stability relative to gamhepathiopine [1].

Takinib (EDHS-206) is a specific and effective TAK1 inhibitor(IC50= 9.5 nM).

Artemether (CGP 56696) is an antimalarial agent used to treat acute uncomplicated malaria.

Artesunate (WR-256283) is part of the artemisinin group of drugs that treat malaria. It is a semi-synthetic derivative of artemisinin that is water-soluble and may therefore be given by injection. It is on the World Health Organization's List of Essential Medicines.

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).

The NPNA hexamer, a peptide, holds potential for malaria research and the development of a sporozoite vaccine [1].

Carpaine, an alkaloid isolated from Carica papaya Linn, has anti-thrombocytopenic activity. It has the anti-plasmodial activity to prevent malaria.

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

Ga(III)protoporphyrin-IX, a model for interporphyrin interactions in malaria pigment, possesses potent antibacterial effects against gram-negative, gram-positive, and acid-fast bacteria. It exhibits high solubility in methanol (MeOH) and serves as a malarial pigment analogue for drug development, as well as a potential antibacterial agent.

1. Pseudoginsenoside RT5 has anti-epilepsy, anti-depressant activity by promoting nerve growth and improve cognitive ability. 2. Pseudoginsenoside RT5 has anti-bacterial, anti-tumor and anti-malaria activities.

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