Antiparasitics

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)