Antiparasitics

Urethane (Ethylurethane) was an antineoplastic agent .Now is used for other medicinal purposes.

Santonin (alpha-Santonin) is a potent antiparasitic agent.

Fenpyroximate is an acaricide and insecticide. It blocks the mitochondrial electron transport in complex I.

Spirodiclofen (BAJ-2740), a selective acaricide from tetronic acid, resists cross-resistance, has insecticidal properties.

Chloroquine: antimalarial, anti-inflammatory, autophagy/TLRs inhibitor, treats arthritis, effective against COVID-19 in vitro. EC50: 1.13 μM.

Xanthatin exhibits cytotoxic, antibacterial, antifungal properties, may treat NSCLC, and inhibits melanoma by targeting Wnt/β-catenin and angiogenesis.

Applications 5-FOA has become a valuable tool for research in the field of molecular genetics. It has been employed in the selection of resistant strains of Saccharomyces cerevisiae that possess a mutant URA3 gene which renders them orotidine-5'-phosphate decarboxylase deficient. 5-FOA is coverted to 5-fluorouridine monophosphate (5-FUMP) in yeast cells, which can become incorporated into RNA or metabolized to the highly toxic 5-fluoro-2’-deoxyuridine monophosphate (5-FdUMP). 5-FdUMP is a potent inhibitor of thymidylate synthase (TS), causing the cessation of DNA synthesis. More recently, 5-FOA has been shown to possess potent antimalarial activity against both chloroquine-susceptible and chloroquine-resistant clones of Plasmodium falciparum. Studies indicate that TS is the primary target of 5-FOA in m References Winston, F., et al.: Genetics, 107, 179 (1984); Boeke, J.D., et al.: Methods Enzymol., 154, 164 (1987); Rathod, P.K., et al.: Antimicrob. Agents Chemother., 33, 1090 (1989); Rathod, P.K., et al.: Antimicrob. Agents Chemother., 36, 704 (1992); Gomez, Z.M . and Rathod, P.K.: Antimicrob. Agents Chemother., 34, 1371 (1990); Gassis, S. and Rathod, P.K.: Antimicrob. Agents Chemother., 40, 914 (1996)

MCG-02 is an inhibitor of cruzain (CRZ) and cathepsin L-like protease (CATL), capable of inhibiting CRZ in Trypanosoma cruzi and CATL in Trypanosoma brucei, with IC50 values of 0.2 μM and 0.02 μM, respectively.

Artesunate (WR-256283) is part of the artemisinin group of drugs that treat malaria.

Applications Artemisinin (A777500) is an effective antimalarial agent used to treat malaria. Artemisinic Aldehyde is converted into dihydroartemisinic aldehyde by Artemisinic aldehyde Δ11 (13) reductase (DBR2), which is involved in the biosynthetic pathway of artemisinin in Artemisia annua L. References Yuan, Y., et al.: Biotechnol Appl Biochem 62, 17 (2015); Arjen, M. D., et al.: N Engl J Med 361, 455 (2009)

Diloxanide (RD3803) is an endomoeba insecticide.

Fenitrothion (Arbogal) is a insecticide that exhibits reproductive toxicity, inhibits acetylcholinesterase, and is commonly used in agriculture.

Inhibits methionine aminopeptidase-2; anti-angiogenic; antibiotic

Phosalone is an organophosphate chemical commonly used as an insecticide and acaricide.

Lotilaner is a parasiticide.

Pyrantel tartrate (Banminth) is broad spectrum anthelmintic for livestock.

Propargite is a pesticide used to kill mites.

Applications A Levamisole derivative References Lewis, J., et al.: Mol. Pharmacol., 31, 185 (1987),

1.(-)-Fucose (6-Desoxygalactose) can anti-infective, anti-cancer, enhance immunity 2.

Diethylcarbamazine citrate treats filariasis, targeting W. bancrofti and L. loa by inhibiting arachidonic acid in microfilaria.

NSC-5844 (RE-640) (RE640) is a bisquinoline compound with C-C chemokine receptor type 1 (CCR1)-agonistic activities.

Clofentezine (Apollo) is an active substance of plant protection product used as the pesticide, acaricide.

Applications Cletoquine is a metabolite of Hydroxychloroquine (H916900), an antimalarial; antirheumatic; lupus erythematosus suppressant. References Yarden, Y., et al.: Nature, 323, 226 (1986); Seifert, R., et al.: J. Biol. Chem., 264, 8771 (1989); Gahl, W., et al.: Mol. Genet. Metab., 76, 234 (2002); Card, J., et al.: Toxicol. Sci., 75, 169 (2003)

Applications Anhydrodihydroartemisinin is a semisynthetic derivative of Artersiminin (A777500). Anhydrodihydroartemisinin is a decomposition product of Artesunate (A777800) and Dihydroartemisinin (D448360). Anhydrodihydroartemisinin showed antimalarial activity although much weaker than its parent compound. References Haynes, R.K. et al.: ChemMedChem, 2, 1448 (2007); Lin, A.J. et al.: Am. J. Trop. Med. Hyg., 50, 777 (1994); Galal, A. et al.: J. Nat. Prod., 68, 1274 (2005);

Fervenulin, from Streptomyces sp. CMU-MH021, halts egg hatch (MIC: 30 μg/mL) and kills J2 larvae (MIC: 120 μg/mL) of M. incognita.

Asparagusic acid is unique to asparagus.

Fumagillin (Amebacilin) is a selective and potent irreversible inhibitor of Methionine aminopeptidase 2 (MetAP2), used as an antibiotic to treat

Furaltadone hydrochloride (Furaltadone HCl) is an antibacterial and shows distinct curative effect in the treatment of coccidiosis.

Gypsogenic acid, a triterpenic acid isolated from Miconia stenostachya, exhibits antibacterial and antitrypanosomal activities. This compound demonstrates minimum inhibitory concentrations (MICs) ranging from 50-200 μg/mL against oral bacterial pathogens including Enterococcus faecalis, Streptococcus salivarius, Streptococcus sanguinis, Streptococcus spp., and Streptococcus sobrinus. Additionally, gypsogenic acid can induce the lysis of Trypanosoma cruzi in isolated mouse blood, with an IC50 value of 56.6 μM.

Artelinic acid is an artemisinin analog with antimalarial activity and is used for the treatment of multi-drug resistant strains of Plasmodium falciparum.

Aklomide (2-Chloro-4-nitrobenzamide) is used in poultry to treat parasites.

PfDHODH-IN-2: powerful antimalarial, blocks PfDHODH (IC50: 1.11 μM), for malaria research.

Stability Light Sensitive Applications Aminorex and Rexamino as metabolites of Levamisole (L331100). References Poos, G., et al.: J. Med. Chem., 6, 266(1963), Watson, A., et al.: Res. Vet. Sci., 45, 411 (1988), Russell, B., et al.: Pharmacol. Biochem. Behav., 51, 375 (1995),

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Oxibendazole: a benzimidazole antiparasitic for horses and pets against various worms.

Moxidectin (CL301423) is an anthelmintic for heartworm/intestinal worms in dogs, cats, horses, cattle, and sheep; oral/topical/injectable.

λ-Cyhalothrin (Icon) is a type II synthetic pyrethroid insecticide featuring a high-efficiency, broad-spectrum formula with an α-cyano group.

Dehydroemetine, a synthetic emetine, treats amoebic infections and leishmaniasis, and resists metronidazole amoebiosis.

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.