BPH-715 is a bisphosphonate, inhibits Plasmodium liver-stage growth, with an IC50 of 10 μM for Plasmodium exoerythrocytic forms in HepG2 cells[1].
Praziquantel D11 is the deuterium labeled Praziquantel, which is an anthelmintic.
Ornidazole(Ro 7-0207) is a 5-nitroimidazole derivative with antiprotozoal and antibacterial properties against anaerobic bacteria. Target: Antibacterial; AntiparasiticOrnidazole is a drug that cures some protozoan infections. Ornidazole 1 g/day is effective for the prevention of recurrence of Crohn's disease after ileocolonic resection [1]. Ornidazole is converted to reduction products that interact with DNA to cause destruction of helical DNA structure and strand leading to a protein synthesis inhibition and cell death in susceptible organisms [2].
KDU731, an orally active C. parvum PI4K inhibitor with an IC50 value of 25 nM, blocks Cryptosporidium infection in vitro and in vivo[1][2]. KDU731 is a promising drug candidate for the treatment of diarrhea caused by Cryptosporidium and meets a broad range of safety[2].
PF 1022A is a N-methylated cyclooctadepsipeptides (CODPs) with strong anthelmintic properties; acts as an ionophore.IC50 value:Target: PF 1022A showed strong anthelmintic activities against Ascaridia galli in chickens [1]. PF1022A is a novel anthelmintic that binds to the latrophilin-like transmembrane receptor important for pharyngeal pumping in nematodes. Furthermore, PF1022A binds to GABA receptors, which might contribute to the anthelmintic effect. Like other cyclodepsipeptides, PF1022A acts as an ionophore [2]. In vitro, PF1022A showed low activity on embryonation but significantly inhibited egg hatch (10 and 100 μg/ml), whereas albendazole (10 and 100 μg/ml) revealed statistically significant inhibitions of both embryonation and egg hatch. PF1022A (1-100 μg/ml) completely inhibited larval movement at most examination points [3].
Broxyquinoline is an antiprotozoal agent.
Ethopabate is an antiprotozoal agent which has been widely used to treat and prevent coccidiosis in chickens.
Avermectin B1 (Abamectin) is a widely used insecticide and anthelmintic. IC50 Value: N/ATarget: AntiparasiticAvermectin B1 is a mixture of avermectins containing more than 80% avermectin B1a and less than 20% avermectin B1b. These two components, B1a and B1b have very similar biological and toxicological properties. The avermectins are insecticidal and antihelmintic compounds derived from various laboratory broths fermented by the soil bacterium Streptomyces avermitilis. Avermectin B1 is a natural fermentation product of this bacterium.
Cratoxylone, isolated from the bark of Cratoxylum Cochinchinense, possesses antiplasmodial activity[1][2].
Fexinidazole is a 5-nitroimidazole drug currently in clinical development for the treatment of human sleeping sickness (human African trypanosomiasis [HAT]), caused by infection with species of the protozoan parasite Trypanosoma brucei. Target: Antiparasiticin vivo: Fexinidazole shows dose-related efficacy in the T. b. rhodesiense (STIB900) acute mouse model at intraperitoneal (i.p.) doses of 20 to 50 mg/kg/day and oral (per os [p.o.]) doses of 25 to 100 mg/kg/day given on four consecutive days, with 100 mg/kg/day p.o. being 100% curative. Fexinidazole is shown to be effective in the GVR35 mouse model, which mimics the advanced and fatal stage of the disease, when parasites have disseminated into the brain. [1]
Phenothrin is a synthetic pyrethroid that kills adult fleas and ticks. It has also been used to kill head lice in humans.
Tafenoquine (WR 238605) is an 8-aminoquinoline. Tafenoquine is an anti-malarial prophylactic agent[1].
Temefos is an organophosphate larvicide, used to treat water infested with disease-carrying insects including mosquitoes, midges, and black fly larvae. Temefos affects the central nervous system through inhibition of cholinesterase, results in death before reaching the adult stage.
Ivermectin is a widely used antiparasitic agent in human and veterinary medicine. It is a positive allosteric effector of P2X4 and the α7 neuronal nicotinic acetylcholine receptor (nAChRs).
Hydroxychloroquine sulfate is a synthetic antimalarial drug which can also inhibit Toll-like receptor 7/9 (TLR7/9) signaling.
Tafenoquine Succinate (WR 238605 Succinate) is an 8-aminoquinoline. Tafenoquine is an anti-malarial prophylactic agent[1].
Clindamycin phosphate is an antibiotic, which blocks the ribosomes of microorganisms. It is usually used to treat infections with anaerobic bacteria, can also be used to treat protozoal diseases, such as malaria.
Clorsulon is used in the treatment of Fasciola hepatica infections in calves and sheep.Target: AntiparasiticClorsulon is a competitive inhibitor of both 3-phosphoglycorate and ATP and had a Ki of 0.29 mM, inhibits glucose utilization and acetate and propionate formation by mature Fasciola hepatica in vitro. [1] Clorsulon (a single dose of 15 mg/kg) is effective in removing over 90% of immature Fasciola hepatica from sheep (6 weeks after infection) and calves (8 weeks after infection). A 2.5 mg/kg dose removed over 90% of mature (16 weeks old) liver fluke from sheep [1]. Clorsulon causes severe disruption to the tegument and gut of Fasciola hepatica after in vivo incubation [2].
Allopurinol riboside, a metabolite of allopurinol, shows potent activities against parasites.
Moxidectin(ProHeart 6; CL301423; Cydectin) is an anthelmintic drug which kills parasitic worms (helminths), and is used for the prevention and control of heartworm and intestinal worms.IC50 value:Target: Anti-parasiticMoxidectin is a semisynthetic derivative of nemadectin, which is produced by fermentation by Streptomyces cyano-griseus. Moxidectin treats and controls some of the most common internal and external parasites by selectively binding to a parasite's glutamate-gated chloride ion channels. These channels are vital to the function of invertebrate nerve and muscle cells; when moxidectin binds to the channels, it disrupts neurotransmission, resulting in paralysis and death of the parasite. Studies of moxidectin show the side effects vary by animal and may be affected by the product’s formulation, application method and dosage.
Avermectin B1a is an antiparasitic agent that paralyzes nematodes without causing hypercontraction or flaccid paralysis.
Broxaldine is an antiprotozoal drug.
Pentamidine(MP-601205) is an antimicrobial agent.Target: AntiparasiticPentamidine has a potent in vitro antiprotozoal activity. Pentamidine displays cytotoxic activity against L. infantum promastigotes with IC50 of 2.5 μM. 2.5 μM Pentamidine induces early programmed cell death in 49.6% of L. infantum promastigotes. 2.5 μM Pentamidine induces a notorious decrease in promastigotes in both G1 and S phases relative to the control-untreated samples (G1:77.0 vs 15.0%; S:11.0 vs 2.4% for control- and pentamidine-treated promastigotes, resp). Pentamidine is able to bind with calf-thymus DNA (CT-DNA) and induces conformational changes in the DNA double helix. Pentamidine also binds with ubiquitin to modifiy the β-cluster of ubiquitin [1]. Pentamidine is an inhibitor of phosphatase of regenerating liver (PRLs). 1 μg/mL of Pentamidine complete inhibits the activity of recombinant PTP1B in dephosphorylating a phos-photyrosine peptide. 10 μg/mL of Pentamidine completely inhibits the activities of recombinant PRL-1, PRL-2 and PRL-3 in dephosphorylating a phosphotyrosine peptide substrate. Incubation with Pentamidine (1 μg/mL) for 48 h reduces the activity of intracellular PRL phosphatases in transfected NIH3T3 cells by more than 85%. 10 μg/mL Pentamidine completely inhibits the growth of melanoma cell line (WM9), prostate carcinoma cell line (DU145 and C4-2), ovarian carcinoma cell line (Hey), colon carcinoma cell line (WM480), and lung carcinoma cell line (A549) which all express endogenous PRLs [2].
(+)-SJ733 is a clinical candidate for malaria which can also inhibit Na+-ATPase PfATP4.
Emetine (dihydrochloride) is an anti-protozoal drug previously used for intestinal and tissue amoebiasis[1].
Oxantel pamoate is a widely available dewormer, potently against Trichuris muris and Hookworms.
Mebendazole is a highly effective, broad-spectrum antihelmintic indicated for the treatment of nematode infestations; has been found as a hedgehog inhibitor.
Bithionol sulfoxide(Bitin-S) is a clinically approved anti-parasitic drug; has been shown to inhibit solid tumor growth in several preclinical cancer models.IC50 value:Target: anticaner agentBithionol caused dose dependent cytotoxicity against all ovarian cancer cell lines tested with IC50 values ranging from 19 μM - 60 μM. BT treatment resulted in cell cycle arrest at G1/M phase and increased ROS generation [1]. Both bithionol and bithionol sulphoxide demonstrated in vitro toxicity to Neoparamoeba spp. at all concentrations examined (0.1 to 10 mg l(-1) over 72 h), with a comparable toxicity to freshwater observed for both chemicals at concentrations > 5 mg l(-1) following a 72 h treatment [2].
Halofantrine hydrochloride (SKF-102886) is a blocker of delayed rectifier potassium current via the inhibition of human-ether-a-go-go-related gene (HERG) channel and a potent antimalarial compound[1][2].
Bephenium hydroxynaphthoate is an anthelmintic agent formerly used in the treatment of hookworm infections and ascariasis; B-type AChR activator.