Antiparasitics

Tizoxanide (Desacetyl-nitazoxanide) is a metabolite of lamivudine.

DCN-83, a potent anti-leishmanial compound, exhibits its highest efficacy against the amastigote form, achieving an IC50 value of 0.71 μM.

Praziquantel (Droncit) is an anthelmintic that paralyzes worms by increasing calcium in muscle cells, causing tegument damage and immune response.

Atovaquone (Atavaquone) is a hydroxynaphthoquinone that has antimicrobial activity and is being used in antimalarial protocols.

Dinitolmide (Zoalene), a poultry feed additive, is a coccidiostat for poultry.

HCQ, an anti-malarial, may induce cancer cell death and is being explored for COVID-19.

Cynaroside (Luteolin 7-O-Glucoside) is a flavone, a flavonoid-like chemical compound. It has an anti-oxidant effect, inhibiting lipid and protein oxidation.

Nitazoxanide (NSC-697855) is a synthetic benzamide antiprotozoal; it disrupts pyruvate electron transfer reactions.

Applications A labelled metabolite of Chloroquine. It is a COVID19-related research product. References Ohkuma, S., et al.: J. Cell. Biol., 90, 656 (1981), Araki, N., et al.: J. Biol. Chem., 267, 10211 (1992), Projean, D., et al.: Drug Metab. Dispos., 31, 748 (2003), Traebert, M., et al.: Eur. J. Pharmacol., 484, 41 (2004),

Cinchonine (LA40221), a potent amide local anesthetic for surface use, is toxic and limited to spinal anesthesia.

Permethrin (NRDC-143) is a pyrethroid insecticide commonly used in the treatment of LICE INFESTATIONS and SCABIES.

Licoflavone B has schistosomicidal activity, it showed high S. mansoni ATPase (IC50 of 23.78 μM) and ADPase (IC50 of 31.50 μM) inhibitory activities.

Imidocarb Dipropionate is an antiprotozoal compound with a mode of action that interferes with the glycolysis of parasites like Babesia. It is used for treating infections such as babesiosis in animals.

Conessine (Conessinum), a steroidal alkaloid isolated from Holarrhena floribunda, interacts with the histamine H3 receptor and has anti-malarial activity.

Applications An intermediate in the preparation of labelled Cletoquine, Chloroquine and respective derivatives References Cavallaro, R., et al.: J. Med. Chem., 42, 2527 (1999), Fellmann, P., et al.: Biochem., 39, 4994 (2000),

OfChi-h-IN-2 (compound TQ19) is a potent inhibitor of OfChi-h, exhibiting a K i of 0.33 μM, and significantly impairs the growth and development of Ostrinia

Amprolium Hydrochloride (Amprolium HCl) is a coccidiostat that interferes with thiamine metabolism.

Clindamycin is a semisynthetic antibiotic that blocks bacterial protein synthesis by detaching peptidyl-tRNA from ribosomes.

UCB7362 hydrochloride (UCB7362 HCl) is an orally active plasmepsin X (PMX) inhibitor (IC50: 7 nM) with antimalarial activity that inhibits parasite growth.

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

Dimetridazole (1, 2-Dimethyl-5-nitroimidazole) is a agent that combats protozoan infections. Dimetridazole is a nitroimidazole class drug.

HAT-IN-8 (Compound 38), a blood-brain barrier-permeable inhibitor of Trypanosoma brucei with an EC50 of 0.18 μM, is utilized in the study of Human African

Sulfachloropyrazine sodium(Sulfachloropyrazine) is an antiprotozoal,with antibacterial and anticoccidial effects

Niranthin is a potent anti-leishmanial agent, inhibits the relaxation activity of heterodimeric type IB topoisomerase of L.

Sulfaquinoxaline (Sulfabenzpyrazine) is an antiprotozoal agent.

Satranidazole is an antimicrobial agent that falls under the category of synthetic nitroimidazoles. It is derived from chemical synthesis and is designed to combat infections caused by specific organisms. The mode of action involves the reduction of the nitro group within the organism, creating reactive intermediates that disrupt DNA synthesis and lead to cell death. This mode of action is notably effective against protozoal infections and anaerobic bacterial infections. Satranidazole's applications primarily include the treatment of parasitic diseases such as amebiasis and giardiasis, and it is particularly effective in addressing anaerobic bacterial infections often encountered in clinical settings. Due to its targeted mechanism, Satranidazole is valuable in treating conditions where conventional antibiotics might be less effective. Its use in therapeutics highlights the importance of precise molecular intervention in the realm of infectious diseases. Researchers and practitioners utilize Satranidazole for its specific activity and efficacy in treating difficult-to-manage infections.

Sarolaner (PF-6450567) is an orally active and broad-spectrum ectoparasiticide (LC80: 0.3 μg/mL against C. felis and an LC100: 0.003 μg/mL against O. turicata).

Impurity Atorvastatin EP Impurity D Applications O-Methyl Atovaquone (Atorvastatin EP Impurity D) is a Atovaquone derivative that shows protozoacidal activity against Plasmodium falciparum. References Danoun, S., et. al.: Heterocycl. Commun., 5, 343 (1999)

Oxibendazole is a benzimidazole anthelmintic with action on microtubule formation in parasitic worms and is used for treating roundworms, strongyles, and pinworms in horses and pets.

(+)-Isopulegol is a monoterpenoid from Mentha canadensis L.

Amitraz (NSC 324552): white monoclinic crystals, mp 86-87°C, water-insoluble, used as acaricide and in canine demodectic mange.

MED6-189, an analog of kalihinol, disrupts the apicoplast functions and vesicular transport in the malignant malaria parasite (P. falciparum, IC50 < 50 nM). The compound specifically targets the apicoplast, which is a non-photosynthetic plastid essential for isoprenoid synthesis, found in most apicomplexan parasites.

ZY-19489: Antimalarial, potential single-dose cure, FDA orphan drug status.

Cysteine protease inhibitor-3 (Compound 15), a cysteine protease inhibitor, exhibits anti-plasmodial activity, effectively inhibiting Pf3D7 (IC50 = 0.74 μM),

Applications Pseurotin A shows antiparasitic and anticancer activity. It exhibits inhibition towards IgE (immunoglobin E) production. References Martinez-Luis, S. et al.: Nat. Prod. Comm., 7, 165 (2012); Bioorg. Med. Chem. Lett., 19, 1457 (2009);

Quinine hydrochloride dihydrate (Quinine HCl Dihydrate) is a white crystalline K+ channel blocker, used to treat malaria.

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

Applications Aminorex is a metabolite of Levamisole (L331100). Aminorex is an anorectic stimulant drug of the 2-amino-5-aryl oxazoline class. Aminorex has been shown to have locomotor stimulant effects similar to Methamphetamine (M258795). 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),