Antiparasitics

Bitoscanate (PDITC) is used in the treatment of hookworms.

Kaempferol (Robigenin) is a natural flavonoid and an inverse agonist of ERRα and ERRγ.

CP-320626 is an effective human liver glycogen phosphorylase (GP) inhibitor with cholesterol-lowering activity, used in type 2 diabetes research.

Ipronidazole (RO-71554) is an orally effective antiprotozoal agent used to prevent and ameliorate histomoniasis in turkeys, commonly referred to as blackhead disease.

Applications Desethyl Chloroquine is the major product of the stereoselective human metabolism of Chloroquine, used for the therapy and prevention of malaria. It is a COVID19-related research product. References Essien, E., et al.: J. Pharm. Pharmacol., 38, 543 (1986), Akintonwa, A., et al.: Ther. Drug Monit., 10, 147 (1988), Boelaert, J., et al.: AIDS, 15, 2205 (2001), Basco, L., et al.: Antimicrob. Agents Chemother., 47, 1391 (2003),

Flubendazole is a benzimidazole anthelmintic with action on microtubule formation in parasites and is used for treating intestinal worms in humans and animals.

Arohynapene B is an anticoccidial compound that inhibits the growth of Eimeria parasites.

Parbendazole (SKF 29044) is a potent inhibitor of microtubule assembly(EC50 : 8.79 nM).Parbendazole is a carbamate ester-amine.

Hexadecylphosphocholine, better known as miltefosine, belongs to the group of phospholipids. The long alkyl chain and a polar group of a molecule proved to be essential for antitumor activity, especially to cure breast cancer cells. The apoptotic process takes place in the plasma membrane, where molecules are inserted and then influence signaling pathways. Moreover, during preclinical studies hexadecylphosphocholine (He-PC) found to be highly effective in inhibiting the growth of chemically induced rat mammary carcinomas, and even a high percentage of the tumors regressed completely. The He-PC has many more applications such as antifungal agent, antiprotozoal drug, protein kinase inhibitor or immunomodulator. Even though miltefosine was originally developed in the 1980s as an anti-cancer agent, new studies have demonstrated activity against Leishmania parasites and neoplastic cells, and due to broad spectrum of antimicrobial effects, it is recommended as a first line treatment for free-living amebae infections.

Applications 2-[[(4S)-4-[(7-chloro-4-quinolinyl)amino]pentyl]ethylamino]-ethanol is the (S) enantiomer of (R)-Hydroxychloroquine (C373710).

DHC curbs antibody and cell-mediated allergies, inhibits mitochondrial potential in macrophages, and has antinociceptive, anti-inflammatory effects.

Tinidazole is a nitroimidazole antibiotic with action on DNA synthesis disruption in anaerobic bacteria and protozoa and is used for treating infections like giardiasis, amebiasis, and trichomoniasis.

Oxysanguinarine (Hydroxysanguinarine) possesses antiplatelet aggregation activity, it has potential inhibitory properties against the dengue virus.

Crotamiton (Eurax) is an antipruritic and a scabicidal agent available as a lotion or cream for topical use only.

Applications 1-Chlorodecane is a reagent in the preparation of antimycobacterial agents. Also used in the synthesis of antimalarial atovaquone derivatives. 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 Pathak, A. et al.: Bioorg. Med. Chem., 21, 1685 (2013); El Hage, S. et al.: Eur. J. Med. Chem., 44, 4778 (2009);

Treatment for leishmaniasis

Pentamidine is an antifungal and antiprotozoal agent, interacting directly with the pathogen genome by binding to AT-rich regions of duplex DNA and the minor

Nifurtimox (BAY-A-2502) is an antiprotozoal agent (IC50s = 9.91, 12.28, and 10.44 μM against Taluahuén, LQ, and Brener strains of T.

Naturally produced by the soil bacterium Streptomyces avermitili, it is clinically used in the treatment of parasitosis in both humans and animals. Ivermectin is commercially available as a mixture of 80% 22, 23-dihydroavermectin B1a and 20% 22, 23-dihydroavermectin B1b. In 2020, Ivermectin indicated that it was a good antiviral agent in the treatment of SARS-CoV-2 and a new mechanism of action has been suggested. Ivermectin would act on importin α/β heterodimer and affect nuclear transport and the translocation of viral proteins.

Toltrazuril (Toltrazurilo), an antiprotozoal agent, has effect on Coccidia parasites.

Hypocrellin A is a natural PKC inhibitor with light-induced antitumor, antifungal and antiviral activities.Cost-effective and quality-assured.

Nepodin exhibits antimalarial, anti-inflammatory, and antidiabetic effects by inhibiting COX and activating AMPK to stimulate GLUT4.

Anthelvencin A is a pyrrolylamide metabolite with moderate antibacterial and anthelmintic activity.

AQ-13 dihydrochloride is an antimalarial drug. It is effective against drug-resistant strains of Plasmodium falciparum.

α-Thujone is an inhibitor of ACh with an IC50 value of 24.7μM.

Applications Ethaverine is an analogue of Papaverine (P190500), an antispasmodic. An isoquinoline derivative with the potential for antimicrobial, antimalarial and cytotoxic antiviral agents. References Kaplan, D., et al.: Biochem. J., 201, 605 (1982), Hifnawy, M.S., et al.: Anal. Profiles Drug Subs., 17, 367 (1988); Iwasa, K. et al.: Bioorg. Med. Chem., 9, 2871 (2001);

CWHM-1552 is an effective Plasmodium falciparum inhibitor. For the 3D7 and Dd2 strains, the IC50s are 51 nM and 53 nM.

Cloxiquine (Dermofongin) is a monohalogenated 8-hydroxyquinoline with activity against bacteria, fungi, and protozoa.

Eugenitin, a polyketide from Mycoleptodiscus indicus, exhibits inhibitory activity against Leishmania major with an LD50 of 39.9 μM and demonstrates low

Quinidine is a stereoisomer of the antimalarial agent quinine and a class Ia antiarrhythmic agent. for the treatment of abnormal heart rhythms and also malaria.

Fluralaner (A1443) is an isoxazoline ectoparasiticide.

Nitroxynil is an anthelmintic for adult/immature parasites, mainly used in Fasciola hepatica studies.

Antileishmanial agent-31 (Compound p1) is a pyrazole derivative exhibiting antileishmanial activity with an IC50 of 35.53 μg/mL. Furthermore, Antileishmanial agent-31 demonstrates high stability and is applicable in studies focused on leishmaniasis treatment.

Eflornithine hydrochloride hydrate (DFMO hydrochloride hydrate) is an ornithine decarboxylase (ODC) inhibitor with antitumor activity. Cost-effective and quality-assured.

2-Benzoxazolinone (2-Hydroxybenzoxazole) is found in cereals and cereal products. 2-Benzoxazolinone is found in rye seedlings.

Hydroxychloroquine sulfate (Acidum iopanoicum) inhibits plasmodial heme polymerase.

Impurity Atovaquone EP Impurity C, Atovaquone USP Related Compound A Applications (±)-Atovaquone Impuriyy C (Atorvastatin EP Impurity C), is the impurity of Atovaquone (A793500), which belongs to the class of naphthoquinones, that inhibits mitochondrial electron transport. It is an Antipneumocystic. References Hudson, A.T., et al.: Drugs Exp. Clin. Res., 17, 427 (1991), Fry, M., et al.: Biochem. Pharmacol., 43, 1545 (1992), El-Sadr, W.M., et al.: N. Engl. J. Med., 339, 1889 (1998),

1.

Dixanthogen (Auligen) is an ectoparasiticide. Dixanthogen is a thiocarbonyl compound.

Pentamidine dihydrochloride (MP-601205 dihydrochloride) is an aromatic diamidine agent with activity against a number of microorganisms including protozoa (

Applications (E)-Cefodizime can be obtained from Ethyl Acetate (E899545) which is a chemical intermediate used in the production of various analgesics, antibiotics and antimalarial agents. References Mutti, F.G., et al.: Adv. Syn. Cata., 354, 3409 (2012); Subudhi, B., et al.: Bull. Chem. Soc., Ethiopia., 26, 455 (2012);

Antileishmanial agent-24 (compound 33) exhibits antileishmanial activity, demonstrating an inhibitory concentration 50 (IC50) value of 5.39 μM against

Conoidin A is a cell permeable inhibitor of T.

INE963: Potent against Pf 3D7 (EC50=6nM), clears parasites in <24h; effective on P. falciparum/vivax isolates (EC50=0.01-7nM).

Applications (2R,3R)-Benzhydryl 2,3-bis(benzyloxy)-4-hydroxybutanoate is an intermediate in synthesizing 4-Phospho D-Erythronate (P355000), which is an intermediate in the synthesis of pyridoxal 5'-phosphate in some bacteria and an inhibitor of ribose 5-phosphate isomerase. Phosphorylated aldonic acids are strong inhibitors of 6-phosphogluconate dehydrogenase, and 4-phospho-D-erythronate (4PE) and 4-phospho-D-erythronohydroxamate are two of the strongest inhibitors of the Trypanosoma brucei enzyme. References Tanaka, N., et al.: J. Mol. Biol., 324, 519 (2002); Fitzpatrick, T., et al.: Biochem. J., 407, 1 (2007); Kalliri, E., et al.: J. Bacteriol., 190, 3793 (2008)

Insecticidal agent 16 (compound A21) exhibits insecticidal activity against Plutella xylostella, with LC50 values of 1.2 and 13.2 µg/mL respectively.

Ac-Atovaquone, an ester-acetylated derivative of atovaquone, acts as a potent inhibitor of cytochrome bc1 (cytochrome bc1). This compound shows potential for use in malaria research.

Bacopasaponin C may have antioxidant activity, it also shows anti-leishmanial property.

Applications 4-Amino-1-pentanol-d4 Benzyl Ether 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),

Applications Piperaquine-d6, is a 4-aminoquinoline derivative used as an antimalarial agent. Piperaquine interferes with physiological function of the food vacuole membrane of the trophozoites leading to autophagocytosis of the parasites. It is commonly used in combination with Dihydroartemisinin (D448360) for the treatment of multi-drug resistant falciparum malaria. References Nguyen, T.M.T. et al.: Tap Chi Duoc Hoc, 57, 22 (2007); Song, J. et al.: Malaria J., 10, 231 (2011);

Halofuginone (RU-19110) inhibits prolyl-tRNA synthetase (Ki=18.3 nM), down-regulates Smad3, and blocks TGF-β at 10 ng/ml.

Applications 5-(N-Ethyl-N-2-hydroxyethylamino)-2-penthlamine is a useful synthetic intermediate in the synthesis of Hydroxy Chloroquine (H905300/H905305); a major metabolite of Chloroquine (C379965, diphosphate salt) which is a standard anti-malarial drug. 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 Brocks, D., et al.: Clin. Pharmacokinet., 42, 1359 (2003); Brocks, D., et al.: Clin. Pharmacokinet., 42, 1359 (2003); Huang, S., et al.: Talanta, 64, 887 (2004); 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)

Applications Cis isomer of Atovaquone-d5.

Trans-Clopenthixol dihydrochloride ((E)-Clopenthixol dihydrochloride), an antibiotic without neuroleptic effects, has demonstrated in vitro efficacy against Pseudomonas aeruginosa and Plasmodium falciparum, as referenced in [1] [2].

Atherosperminine inhibits AChE/BChE and relaxes trachealis via cAMP phosphodiesterase inhibition.

Piperonyl butoxide (Pyrenone 606) is an insecticide synergist, particularly for rotenone and pyrethroids.

Antileishmanial agent-21 (compound 4e) functions as an inhibitor of Leishmania pteridine reductase 1 (Lm-PTR1), employing an anti-folate mechanism.

UCB7362 (GLXC-26743) is an orally available and potent plasmepsin X (PMX) inhibitor with anti-malarial activity.UCB7362 inhibits parasite reproduction.

Eflornithine blocks ornithine decarboxylase, treating African trypanosomiasis and female facial hair.

Antileishmanial agent-20 exhibits selectivity against the Leishmania parasite, with IC50 values of 2.8 μM for L.

Kojic acid is a fungal metabolite that inhibits tyrosinase, an enzyme involved in melanin synthesis, with an IC50 value of 30.6 μM for mushroom tyrosinase.

Primaquine is an antimalarial compound and a gametocytocide, clearing liver schizonts and dormant forms of Plasmodium vivax.

Antileishmanial agent-22 (compound 15b) serves as an antiparasitic and antibacterial, exhibiting activities against Leishmania (IC50 = 0.408 μM), malaria, and

Osthole (Osthol), a potential inhibitor of histamine H1 receptor, has been shown to stimulate osteoblast proliferation and differentiation.

Brotianide (BAY-VA4059) has anthelmintic activity and is highly potent against liver fluke and gastric fluke infestations and can be used to treat acute,