Antiparassitari

Applications 1,4-Dichloro-2,5-bis(trichloromethyl)-Benzene is a derivative compound of 1,4-Bis(trichloromethyl)-2-chlorobenzene (B585580), that acts as a reagent for the synthesis of hexachloroxylene derivatives which functions pharmaceutically as antimalaria and as a schistosomicides.
References Elslager, E., et al.: J. Med. Chem., 13, 542 (1970)

Applications Quininone has been shown to have antimalarial activity in mice. Quininone has been shown to aid the binding of drug-induced antibodies to human platelets.
References Klayman, D.L., et. al.: J. Med. Chem., 16, 1042 (1973); Christie, D.J., et. al.: J. Lab. Clin. Med., 104, 730 (1984)

Applications 5-Bromo-1,2,3-trichlorobenzene is a useful intermediate in the preparation of isoxazole derivatives for controlling parasites, such as Rhipicephalus sanguineous nymphs.
References Gauvry, Noelle., et al.: PCT Int. Appl., WO 2012120135 A1 20120913. (2012);

Applications rac-Febrifugine dihydrochloride is the salt of Febrifugine, a bioactive constituent of a Chinese medicinal herb that is characterized by its therapeutic activity regarding malaria, cancer, fibrosis and inflammatory diseases.
References Keller, T.L.: Nat. Chem. Bio., 8, 311, (2012); Zhu, S. et al.: Bio. Med. Chem., 17, 4496 (2009);

Applications Diclazuril 6-Carboxylic Acid is an impurity of Diclazuril (D436200), a nucleotide analog with broad-spectrum anticoccidial activity.
References Fodey, T.L., et al.: J. Immunol. Meth., 323, 31 (2007);

Impurity Ivermectin EP Impurity K
Applications 3,4-Dihydro Ivermectin 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

Applications 4-Phospho-D-erythronate 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),

Applications Diclazuril 6-Carboxylic Acid [(4-Chlorophenyl)cyanomethyl]-2,6-dichlorophenyl-4-amide is an dimerized impurity of Diclazuril (D436200), a nucleotide analog with broad-spectrum anticoccidial activity.

Applications 4-Methoxy-6-(2-phenylethyl)-2H-pyran-2-one is a Kawain (K145490) derivative that is known to exhibit antimalarial and antituberculosis activities. 4-Methoxy-6-(2-phenylethyl)-2H-pyran-2-one has been identified as a lead compound for the dual treatment of malaria and leishmaniasis.
References McCracken, S.T., et al.: Bioorg. Med. Chem., 20, 1482 (2012); Elzaawely, A.A.. et al.: Food. Chem., 103, 486 (2007); Xuan, T.D., et al.: J. Natural. Med., 62, 188 (2008);

Applications Piperazine Dihydrochloride is an anthelmintic agent used in the treatment of parasitic worms in animals.
References Boes, J.et al.: Vet. Parasitol., 75, 181 (1998); Praslicka, J. et al.: Int. J. Parasitol., 27, 1523 (1997);

Stability Moisture Sensitive
Applications N-(2-Benzoyl-4-chlorophenyl)formamide is used as a reagent in the synthesis of 2-aminoindole compounds that can be used as antimalarial agents.
References Mazitschek, R., et al.: PCT Int. Appl. WO 2011053697 A1 20110505. May 5, 2011

Applications 4-Dechloro-4-hydroxy Diclazuril is an impurity of Diclazuril (D436200), a nucleotide analog with broad-spectrum anticoccidial activity.
References Fodey, T.L., et al.: J. Immunol. Meth., 323, 31 (2007);

Applications A diaminopyrimidine derivative with antimalarial and antibacterial properties.
References Coats, E. et al.: Eur. J. Med. Chem., 14, 261 (1979); Falco, E. et al.: Brit. J. Pharmacol. Chemoth., 6, 185 (1951)

Applications Used in the antileishmanial activity of lipidic amino alcohols.
References Coimbra, E.: Chem. Biol. Drug Des. 75, 233 (2010).

Applications Diclazuril 6-Carboxamide is an impurity of Diclazuril (D436200), a nucleotide analog with broad-spectrum anticoccidial activity.

Applications 2-(Aminomethyl)-4-((7-chloroquinolin-4-yl)amino)phenol is a metabolite of Amodiaquine (A634200), an antimalarial agent.
References Mariga, S.T., et. al.: Acta Tropica, 93, 221 (2005); Natarajan, L., et al.: Arzneim.-Forsch., 22, 1230 (1972); Kracmer, J., et al.: Pharmazie, 29, 773 (1974); Ahmad, I., et al.: Anal. Profiles Drug Subs., 21, 43 (1992)

Applications An intermediate in the synthesis of nicotinamide with potential anticoccidial activity.
References Morisawa, Y. et al.: J. Med. Chem., 20, 129 (1977);

Applications Alloc Bromoridane is used as an anticoccidial agent. Alloc Bromoridane is an intermediate of Febrifugine and Halofuginone (H102500), as inhibitors of prolyl-tRNA synthetase.

Applications 5-O-Demethyl-28-oxo-Avermectin A1a is a derivatie of Ivermectin (I940800), which is a semi-synthetic derivative of Abamectin. An invitro inhibitor of SARS-CoV-2/ Covid-19.
References Chabala, J.C., et al.: J. Med. Chem., 23, 1134 (1980); Campbell, W.C., et al.: Science, 221, 823 (1983); Bennett, J.L., et al.: Parasitol. Today, 4, 226 (1988); Plaisier, A.P., et al.: J. Infect. Dis., 172, 204 (1995);; Caly, L., et al.: Antivir. Res., 178

Stability Hygroscopic
Applications The antibiotics Fosmidomycin and FR900098 are members of a unique class of phosphonic acid natural products that inhibit the nonmevalonate pathway for isoprenoid biosynthesis. Both are potent antibacterial and antimalarial compounds.
References Altschul, S., et al.: J. Mol. Biol., 215, 403 (1990), Altschul, S., et al.: J. Mol. Biol., 215, 403 (1990), Noda, M., et al.: J. Biol. Chem., 279, 46143 (2004), Snow, R., et al.: Nature, 434, 214 (2005),

Stability Light Sensitive
Applications Aminorex and Rexamino as metabolites of Levamisole (L331100).
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),

Applications Gossypol is a mixture of natural polyphenols isolated from the cotton plant. It causes spermatogenesis arrest in humans and also functions as an anti-malarial agent. Antiinflammatory. Anticancer.
References Huo, M. et al.: Int. Immunopharmacol., 15, 442 (2013); Coutinho, E. et al.: Contraception. 65, 259 (2002); Royer, R. et al.: J. Med. Chem., 29, 1799 (1986);

Impurity Metoclopramide EP Impurity E
Applications 2-Diethylaminoethylamine (Metoclopramide EP Impurity E) is used in the syntheses of anti-malarials. In addition, it has been seem to induce apoptosis through a caspase-3 dependent pathway.
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 Kumar, S. et al.: MedChemComm, 3, 489 (2012); del Olmo, E. et al.: Bioorg. Med. Chem. Lett., 12, 2621 (2002);

Applications Monepantel is a recently discovered anthelmitic used in the treatment of parasitic nematodes via stun or kill without damaging the host entity.
References Baur, R. et al.: Mol. Pharm., 87, 96 (2015); Stuchlikova, L. et al.: Chemico. Biol. Interact., 227, 63 (2015);

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

Treatment for leishmaniasis

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.

Primaquine is an antimalarial agent with action on Plasmodium hypnozoites in the liver and is used for preventing relapses of malaria caused by Plasmodium vivax and Plasmodium ovale.

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.

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.

Applications (2R,3R)-Benzhydryl 2,3-Bis(benzyloxy)-4-((bis(benzyloxy)phosphoryl)oxy)butanoate 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)

Applications Antimalarial agent. The compound showed antimalarial activity similar to that of Chloroquine.
References Desjardins, R., et al.: Antimicrob. Agents Chemother., 16, 710 (1979), McKie, J., et al.: J. Med. Chem., 41, 1367 (1998), Gozalbes, R., et al.: J. Pharm. Pharmacol., 52, 111 (1999), Marrero-Ponce, Y., et al.: Bioorg. Med. Chem., 13, 1293 (2005),

Applications Farnesal is a reagent in the synthesis of farnesylpyrophosphate analogues which acts as bisubstrate inhibitors of protein farnesyltransferase and has antiparasitics properties.
References Duez, S. et al.: Bioorg. Med. Chem., 18, 543 (2010);

Applications N-(2-Indol-3-ylethyl)-succinamic Acid Methyl Ester is an intermediate in the synthesis of Canthin-6-one (C175635), which is used as an anticancer agent compromising cancer cells showing multi-drug resistance. Also used in the synthesis of β-carbolinium compounds as antimalarial agents.
References Murakami, C. et al.: Bioorg. Med. Chem., 12, 4963 (2004); Takasu, K. et al.: Chem. Pharm. Bull., 53, 653 (2005);

Applications 4''-Keto-5-O-[(2-propenyloxy)carbonyl]-Abamectin is a derivative of Abamectin (A107000), a mixture of avermectins, containing at least 80% of avermectin B1a (C48H72O14) and not more than 20% of avermectin B1b (C47H70O14). Used as acaricide, insecticide, Cannabis pesticide detection.
References Wang, S., et al.: Prog. Clin. Biol. Res., 97, 373 (1982); Greenblatt, J.A., et al.: J. Agric. Entomol., 3, 233 (1986); Drexler, G., et al.: Eur. J. Pharmacol., 99, 269 (1984);

Applications (6R,13S,25R)-5-O-Demethyl-28-deoxy-5-O-[(1,1-dimethylethyl)dimethylsilyl]-6,28-epoxy-13-hydroxy-25-[(1S)-1-methylpropyl] Milbemycin B is an intermediate used in the synthesis of Milbemycin D (M344290), which is a macrocyclic lactones that can be used as a nematocide and insecticide.
References Arena, J. P., et al.: J. Parasitol 81, 286 (1995); Takiguchi, Y., et al.: J. Antibiot 36, 502 (1983)

Applications N-[[[2-Nitro-5-(propylthio)phenyl]amino]thioxomethyl]carbamic Acid Methyl Ester is an intermediate in the synthesis of Netobimin (N390900), a phenylguanidine anthelmintic agent.
References Hernandez-Luiz, F., et al.: Bioorg. Med. Chem. Lett., 6, 2231 (1996);

Applications 3-Chloro-N-(3-methoxyphenyl)propanamide acts as an inhibitor towards DOXP-reductoisomerase (DXR), a primary target for antimalarial drugs.
References Bodill, T. et al.: Bioorg. Med. Chem., 21, 4332 (2013);

Applications Benzenebutanoic Acid Ethyl Ester is used in the synthesis of thiazolium salts with potent antimalarial activity. Also used in the preparation of novel lactate dehydrogenase A inhibitors. This compound is suitable for lactate dehydrogenase (LDH) related research.
References Hamze, A. et al.: J. Med. Chem., 48, 3639 (2005); Ward, R. et al.: J. Med. Chem., 55, 3285 (2012);

Applications Diethyl Isobutylmalonate is used as a reagent in the synthesis of quinoline-based zinc metallo-aminopeptidase inhibitors which have antimalarial activity.
References Flipo, M., et al.: Bioorg. Med. Chem. Lett., 13, 2659 (2003)

Applications Bruceantin A acts as an anti-babesial quassinoid, extracted from the fruits of Brucea javanica, also an effective anti-trypanosomal agent in vitro. Cytotoxic agent.
References Bawm, S. et al.: Vet. Parasitol., 158, 288 (2008); Elkhateeb, A, et al.: Nat. Prod. Comm., 3, 145 (2008);

Applications 5-Nitro-1H-quinolin-2-one is used in the synthetic preparation of novel antileishmanial agents for Leishmania donovani promastigotes.
References Paloque, L., et al.: Europ. J. Med. Chem., 54, 75 (2012);

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);

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)

Applications α-(3,4-Diethoxyphenyl)-6,7-diethoxy-1-isoquinolinemethanol is an intermediate in synthesizing Ethaverine (E676700), which 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);

Applications A metabolte of the antimalarial endoperoxide Dihydroartemisinin (D448360).
References Maggs, J. et al.: Drug Metab. Dispos., 25, 1200 (1997); Idowu, O.R. et al.: Pharmac. Res., 14, 1449 (1997);

Stability No Date Available
Applications (E)-4-Hydroxycrotonoic Acid Ethyl Ester is an intermediate in the preparation of unusual amino acids that are potential Michael acceptor based antiplasmodial and antitrypanosomal cysteine protease inhibitors.
References Breuning, A., et al.: J. Med. Chem., 53, 1951 (2010);

Applications Artemisic Acid is a derivative of Artemisinin (A777500), an antimalarial constituent of the tradional Chinese medicinal herb Artemisia annua L., Compositae, which has been known for almost 2000 years as Qinghao. Antimalarial.
References Klayman, D.L., et al.: Science, 228, 1049 (1985), Price, R.N., et al.: Expert Opin. Invest. Drugs, 9, 1815 (2000), Meshnick, S.R., et al.: Int. J., Parasitol., 32, 1655 (2002),

Applications 4,4'-Dimethyldiphenylamine is a reagent used in the comparative studies of the analgesic and anti-inflammatory properties of N-phenylanthranilic acids and mefenamic acid, and the anti parasitic activities of some substituted diphenylamines.
References Izard-Verchere, C., et al.: Chimica Therapeutica, 6, 346 (1971)

Applications 6-(Aminocarbonyl)pyridine-3-boronic Acid is a reagent in the identification of highly potent compounds against human malaria parasite Plasmodium falciparum.
References Le Manach, C., et al.: J. Med. Chem., 59, 9890-9905 (2016);