Antiparasitics

Abametapir (BRN 0123183), a metalloproteinase inhibitor, is able to target metalloproteinases critical to egg hatching and louse development.

TMF, derived from M. exotica, shows anti-malarial, fungal, mycobacterial, and anti-inflammatory effects, targeting β-catenin for joint protection.

8-Deoxygartanin is a butyrylcholinesterase (BChE) selective inhibitor, it exhibits significant inhibition of self-induced α2-amyloid (Aα2) aggregation, it has

PIQ-2 (compound 54) serves as an antiprotozoal agent, displaying potent activity against IP. falciparum 3D7 and B. divergens Rouen, with IC50 values of 9.4 nM and 1.6 nM, respectively.

Antimalarial agent 44 (Compound 3) is an antiparasitic agent effective against malaria. It exhibits good permeability in MDCK-MDR1 cell monolayers and has a high clearance rate in mouse liver microsomes.

Avermectin B1a is a macrocyclic lactone disaccharide anthelmintic agent .

PF 1022A is a cyclooctadepsipeptide, which is a type of cyclic peptide composed of amino acids and hydroxy acids. It is derived from the fermentation products of the fungus *Mycelia sterilia*, a member of the *Rosellinia* genus. Its mode of action involves disrupting glutamate-gated chloride channels in parasitic nematodes, which leads to paralysis and eventual death of the parasite. PF 1022A is primarily used for its anthelmintic properties, making it useful for controlling parasitic worm infections in animals. The compound's ability to selectively target nematodes without significant harm to the host organism makes it a valuable tool in veterinary medicine. It serves as a key component in formulations designed to combat gastrointestinal nematodes in livestock and pets, contributing to enhanced health and productivity in affected animals. Research into PF 1022A continues to explore its full potential and further applications in parasitology.

Cipargamin (NITD609) is an effective antimalarial compound. It has an IC50 of appr 1 nM against P. falciparum.

Benznidazole is an antiprotozoal agent and is used for the treatment of Chagas disease. It generates free radicals that damage the DNA and other cellular components of the parasite.

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Nanaomycin A, a quinone antibiotic, reactivates cancer suppressor genes and inhibits DNMT3B (IC50=500nM).

Antimalarial agent 45 (compound 8I) is an antimalarial with activity against Plasmodium parasites, exhibiting an IC50 of 0.21 μM. It is used in the study of malaria.

Ornidazole (Levo-) (Levornidazole) is the levo-isomer of Ornidazole.

Doramectin is a macrocyclic lactone antiparasitic agent with action on glutamate-gated chloride channels in parasites and is used for treating internal and external parasitic infections in livestock.

TSO-13 is an inhibitor of the major cysteine protease Cruzipain found in Trypanosoma cruzi, with an IC50 of 2.2 μM. In Vero cells, TSO-13 also suppresses T. cruzi, exhibiting an IC50 of 1.9 μM.

Fenbendazole (Fenbendazol) is an antinematodal benzimidazole used in veterinary medicine.

Antileishmanial agent-14, a sulfuretin analog, exhibits potential activity against Leishmania donovani promastigotes (IC 50 = 4.1 μM) and inhibits infection by

Fenbendazole is a benzimidazole anthelmintic with action on microtubule formation in parasites and is used for treating gastrointestinal parasites in animals.

Temephos is an organothiophosphate insecticide and cholinesterase inhibitor for treating water with disease-carrying insects.

Antileishmanial agent-23 (compound G1/9), a potent and selective trypanothione reductase (TR) inhibitor, exhibits an IC50 of 2.24 ± 0.52 μM.

D-Phenothrin is a synthetic pyrethroid used in vet medicine for pest control and to kill insects, mosquitoes, and lice.

Amoscanate is an antischistosomal agent, which is a synthetic compound with a broad spectrum of activity against parasitic infections. Its mode of action involves the disruption of parasite metabolism and structure, ultimately leading to the elimination of schistosomes. Schistosomes are trematode worms responsible for schistosomiasis, a significant parasitic disease affecting millions of people worldwide. In terms of its applications, Amoscanate is primarily used in the treatment and management of schistosomiasis, where it targets both the adult and larval stages of the parasite. The synthetic origin of Amoscanate allows for precise adjustments in its chemical structure, optimizing efficacy and minimizing adverse effects. Research on its mechanism indicates that Amoscanate interferes with key biological pathways within the parasite, thereby eradicating the infection. While its current use might be focused on helminthic diseases, ongoing studies aim to elucidate additional therapeutic potential. The growing interest in this compound underscores the need for novel therapies in the treatment of neglected tropical diseases.

Levamisole is a synthetic imidazothiazole derivative belonging to the family of anthelmintic drugs. It is a nicotinic acetylcholine receptor (nAChR) agonists that binds to nAChRs on the neuromuscular junctions of parasitic worms, mimicking the action of the neurotransmitter acetylcholine. This excessive stimulation of nAChRs leads to persistent depolarization of muscle cells and spastic paralysis to expel of the worms. Levamisole exhibits broad-spectrum activity against various roundworms, whipworms, hookworms, and threadworms. Levamisole HCl is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready-to-use products for assay development, screening or other R&D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.

Proguanil hydrochloride, a biguanide, metabolizes into cycloguanil, an anti-malaria agent that inhibits plasmodium's DNA and protein synthesis.

Purvalanol B (NG 95) is a CDK inhibitor that inhibits Cdk2/cyclin A, Cdk2/cyclin E, Cdk5/p35, and Cdk2/cyclin B (IC50s = 6, 9, 6, and 6 nM, respectively)

Applications A labelled Chloroquine metabolite, also an intermediate in the preparation of labelled Chloroquine It is a COVID19-related research product. References Brown, N., et al.: J. Chromatogr., Biomed. App., 309, 426 (1984), Nord, K., et al.: Int. J. Pharm., 72, 11 (1991),

Piperazine adipate is a potent broad spectrum anthelmintic.

Compound 4b (antitrypanosomal agent 13) is a potent antitrypanosomal with notable trypanocidal and cytotoxic activities, exhibiting GI50 values of 0.18 μM

ABMA is a broad-spectrum inhibitor shielding cells from viruses, bacteria, and parasites, acting in late endosomes.

Antileishmanial agent-25 (compound 24) exhibits selective activity against intracellular amastigotes, demonstrating an inhibitory concentration (IC50) of 6.63

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

Cycloguanil hydrochloride, proguanil's metabolite, inhibits Plasmodium/human dihydrofolate reductase (Ki: 0.3/1.5 nM).

Ethylhydrocupreine hydrochloride (Optochin hydrochloride) is a derivative of quinine with antimicrobial activity against Streptococcus pneumoniae.

Hexylresorcinol (4-Hexylresorcinol) is a substituted dihydroxybenzene used topically as an antiseptic for the treatment of minor skin infections.

Amodiaquine dihydrochloride dihydrate (Amodiaquin hydrochloride) is an orally active 4-aminoquinoline derivative with antimalarial and anti-inflammatory effects

Rufigallol, an anthraquinone with six OH groups, induces DLC and fluoresces when aggregated, showing antimalarial effects with vitamin C and ketones.

Imidocarb dipropionate is an antigenic insecticide, is active against the protozoan parasite B. bovis (IC50 : 0.87 μg/ml).

Pyrimethamine (Pirimecidan) is a competitive inhibitor of dihydrofolate reductase (DHFR), used as an antimalarial drug.

Applications An intermediate in the synthesis of the metabolite of Nitazoxanide. References Honma, K., et al.: Chem. Pharm. Bull., 24, 394 (1976), Dubreuil, L., et al.: Antimicrob. Agents Chemother., 40, 2266 (1996), Stockis, A., et al.: Int. J. Clin. Pharmacol. Ther., 34, 349 (1996),

Kukoamine A: anticancer, cytoprotective, antioxidant, anti-inflammatory, inhibits trypanothione reductase (mixed inhibitor, Ki=1.8µM).