Antiparassitari

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.

Chloroquine is a 4-aminoquinolone that is used to prevent and treat malaria, caused by parasitic protozoan from the Plasmodium genus. Chloroquine i a schizonticidal agent and is a widely prescribed antimalarial compound. The antiviral activity of chloroquine in vitro has been reported in 1960’s and recent publications have brought attention to its possible benefits in the treatment of COVID-19 patients, infected with the newly emerged coronavirus (SARS-CoV-2). Current evidence shows that chloroquine inhibits SARS CoV-2 entry in host cells by interfering with endocytosis and affecting the glycoprofile on the S-glycoprotein.

Anti-malarial quinine analogue; effective against Covid-19 infection in vitro

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.

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.

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.

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.

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 (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)