Antiparasitics

Febantel is an anthelmintic. It is used for veterinary use on dogs, cats, cattle, sheep, goats, pig, and poultry against roundworms and tapeworms.

Applications A labelled metabolite of Nitazoxanide (N490100); a potent inhibitor of hepatitis B virus and hepatitis C virus. Kills Mycobacterium tuberculosis. References Allen, M., et al.: Hepatology, 27, 1670 (1998), Blight, K., et al.: Science, 290, 1972 (2000), Blight, K., et al.: J. Virol., 77, 3181 (2003), Courcambeck, J., et al.: Antivir Ther., 11, 847 (2006), Hoffman, P., et al.: Antimicrob. Agents Chemother., 51, 868 (2007); de Carvalho et. al., J. Med. Chem., 52, 5789 (2009)

Epoxyazadiradione, from Neem, may trigger apoptosis and block NF-kB in cervical cancer cells.

Applications Labelled Nitazoxanide. An anthelmintic (cestodes), antiprotozoal (cryptosporidium). Kills Mycobacterium tuberculosis. References Cavier, R., et al.: Eur. J. Med. Chem.-Chim. Ther., 13, 539 (1978), Dubreuil, L., et al.: Antimicrob. Ag. Chemother., 40, 2266 (1996), Stockis, A., et al.: Int. J. Clin. Pharmacol. Ther., 34, 349 (1996), Nathan, C., et al.: J. Med. Chem. 52, 5789 (2009): de Carvalho et. al., J. Med. Chem., 52, 5789 (2009)

PPA-904 is a specific phenothiazine photosensitizer,and used in photodynamic therapy.

Ascomycin (Immunomycin)(Immunomycin, FR-900520, FK520) is an ethyl analog of tacrolimus (FK506) with strong immunosuppressant properties.

Antimalarial agent 28 (Compound 2i) acts as an antiplasmodial agent, exhibiting inhibition of P.

Quinine dihydrochloride (Quinine bimuriate) is a primary alkaloid of various species of Cinchona (Rubiaceae).

Applications o-Chloromethyltoluene is a building block that has been used in the preparation of fenarimol analogs showing curative activity in an experimental model of Chagas disease. Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package References Keenan, M., et. al.: J. med. Chem., 56, 10158 (2013)

Antimalarial agent 46 (Compound 42a) is a compound with antimalarial activity, effective in inhibiting P. falciparum lines.

Applications Enpiroline is an antimalarial agent. Enpiroline showed antischistosomal activity against adult Schistosoma mansoni in mice with Schistosoma mansoni infection. References Ingram, K. et al.: Antimicrob. Agents Chemother., 56, 3207 (2012); Schmidt, L.H. et al.: Antimicrob. Agents CHemother., 14, 420 (1978);

Asiatic acid (Dammarolic acid) is the aglycone of asiaticoside used in wound healing with antioxidant, anti-inflammatory, and neuroprotective properties.

Doramectin (Dectomax) is an antiparasitic agent.

Applications Mefloquine (M207050) labelled intermediate. References Bergqvist Y., et al.: J. Chromatogr., 427, 295 (1988),

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.

Applications An intermediate in the preparation of labelled Cletoquine, Chloroquine and respective derivatives References Ohta, S., et al.: Chem. Pharm. Bull., 34, 4916 (1986), Davis, J., et al.: J. Biol. Chem., 262, 82 (1987),

Flubendazole (Flumoxane) is available OTC in Europe that is an anthelmintic using to treat worm infection in humans.

Hycanthone (Etrenol(mesylate)) is a potent drug of antischistosomal.

Eugenol (Allylguaiacol) is a Standardized Chemical Allergen.

Impurity Ivermectin EP Impurity D Applications 28-Oxo Ivermectin B1a is an impurity of Ivermectin (I940800), an antiparasitic drug that is active against a wide variety of nematode and arthropod parasites and is used to treat scabies and lice in humans. An invitro inhibitor of SARS-CoV-2/ Covid-19. Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package References Campbell, W., et al.: Science, 221, 823 (1983); Glaziou, P., et al.: Trop. Med. Parasitol., 45, 253 (1994); Meinking, T., et al.: New Engl. J. Med., 333, 26 (1995); Caly, L., et al.: Antivir. Res., 178

α-Terpinene is a terpenoid,has acaricidal, antiprotozoal, and antioxidant properties

Applications 4-Amino-1-pentanol-d4 is an intermediate in the synthesis of Hydroxychloroquine-d4 Sulfate (H916902), which is 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),

Aurachin C is a quinoline alkaloid belonging to the isoprenoid class, known for its antimalarial, antifungal, and antibacterial properties. It acts as a selective terminal oxidase inhibitor.

Stability Hygroscopic Applications Standard anti-malarial drug. Substrate for MRP in multidrug resistant cell line and inhibits photoaffinity labelling of MRP by quinoline-based photoactive drug IAAQ. It is a COVID19-related research product. References Luthman, H., et al.: Nucleic Acids Res., 11, 1295 (1983), Vezmar, M., et al.: Biochem. Pharmacol., 56, 733 (1998), Krajewski, W.A., et al.: J. Biomol. Struct. Dyn., 16, 1097 (1999),

Quinidine hydrochloride monohydrate is an optical isomer of quinine. Quinidine prolongs cellular action potential and decreases automaticity.

Emamectin Benzoate (MK-244), by binding gamma-aminobutyric acid (GABA) receptor and glutamate-gated chloride channels disrupting nerve signals within arthropods

Phenothrin (Sumithrin) is a synthetic pyrethroid used to kill adult fleas and ticks.

Buparvaquone (BW 720C) is a hydroxynaphthoquinone antiprotozoal drug related to atovaquone and parvaquone.

Picaridin (Lcaridin) is a topical insect repellent.

Pyridaben is a METI acaricide that inhibits mitochondrial electron transport at complex I (METI; Ki = 0.36 nmol/mg protein in rat brain mitochondria).

DNDI-6148 has anti-experimental cutaneous leishmaniasis activity and can be used to study visceral leishmaniasis.

Toltrazuril sulfone (Ponazuril) is an antiprotozoal agent that acts upon Coccidia parasites.

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Nitromide (3,5-Dinitrobenzamide) is an anti-parasitic drug.

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.