Bruceine A(NSC310616; Dihydrobrusatol) is a natural quassinoid compound extracted from the dried fruits of Brucea javanica (L.); are potential candidates for the treatment of canine babesiosis.IC50 value:Target: Bruceine A inhibited the in vitro growth of Babesia gibsoni in canine erythrocytes at lower concentration compared with the standard antibabesial drug diminazene aceturate and killed the parasites within 24 hr at a concentration of 25 nM. Oral administration of bruceine A at a dosage of 6.4 mg/kg/day for 5 days resulted in no clinical findings in a dog with normal ranges of hematological and biochemical values in the blood. Three dogs were infected with B. gibsoni and two of them were treated with bruceine A at a dosage of 6.4 mg/kg/day for 6 days from day 5 post-infection.
Naphthoquine phosphate is antimalarial drug.IC50 Value: N/ATarget: AntiparasiticNaphthoquine phosphate and artemisinine are two antimalarials developed in China. Both drugs have proven to be efficacious and well tolerated as monotherapy as well as in combination in patients suffering from malaria. The Co-naphthoquine, a novel antimalarial combination, is an oral fixed combination tablet of the naphthoquine phosphate and artemisinine. Artemisinin is characterised by a rapid onset of schizonticidal action and a short half-life. Parasite clearance is, however, often incomplete when it is employed as a single agent unless high dosages are used over several days, but such a regimen may reduce patient compliance and increase the danger of toxicity. Naphthoquine phosphate, by contrast, has a slower onset of action and a longer half-life, associated with a low recrudescence rate.
Crotamiton is a drug that is used both as a scabicidal (for treating scabies) and as a general antipruritic. It is a prescription lotion based medicine that is applied to the whole body to get rid of the scabies parasite.
Warangalone is an anti-malarial compound which can inhibit the growth of both strains of parasite 3D7 (chloroquine sensitive) and K1 (chloroquine resistant) with IC50s of 4.8 μg/mL and 3.7 μg/mL, respectively. Warangalone can also inhibit cyclic AMP-dependent protein kinase catalytic subunit (cAK) with an IC50 of 3.5 μM.
Albendazole is a member of the benzimidazole compounds used as a drug indicated for the treatment of a variety of worm infestations.Target: AntiparasiticAlbendazole, marketed as Albenza (United States), Eskazole, Zentel, Andazol and Alworm, is a benzimidazole drug used for the treatment of a variety of parasitic worm infestations. Although this use is widespread in the United States, the U.S. Food and Drug Administration (FDA) has not approved albendazole for this indication. It is marketed by Amedra Pharmaceuticals. Albendazole was first discovered at the SmithKline Animal Health Laboratories in 1972. It is a broad spectrum anthelmintic, effective against roundworms, tapeworms, and flukes of domestic animals and humans.Albendazole has been used as an anthelmintic and for control of flukes in a variety of animal species, including cattle, sheep, goats, swine, camels, dogs, cats, elephants, poultry and others. In many countries, it is very commonly used for ruminant livestock. For use in livestock, albendazole is marketed by Zoetis (formerly Pfizer Animal Health) in numerous countries (including the United States and Canada) as Valbazen in oral suspension and paste formulations; by Interchemie in the Netherlands and elsewhere as Albenol-100; by Channelle Animal Health Ltd. in the United Kingdom as Albex; by Ravensdown in New Zealand as Albendazole; etc. Although most formulations are administered orally, Ricomax (ricobendazole, or albendazole sulfoxide) is administered by subcutaneous injection.
Nimorazole (K-1900) is a nitroimidazole anti-infective.
Benznidazol (Ro 07-1051) is an antiparasitic medication, with an IC50 of 20.35 μM for Colombian T. cruzi strains, and has been used in the treatment of Chagas disease[1][2].
Primaquine is the only generally available anti-malarial that prevents relapse in vivax and ovale malaria, and the only potent gametocytocide in falciparum malaria.
Fluralaner (INN) is a systemic insecticide and acaricide Fluralaner through potent blockage of GABA and L-glutamate gated chloride channels.
Amprolium is a coccidiostat used in poultry, is a thiamine analogue and blocks the thiamine transporter of Eimeria species by blocking thiamine uptake it prevents carbohydrate synthesis.
Bitoscanate (p-Phenylene diisothiocyanate) is an organic chemical compound used in the treatment of hookworms.
Ornidazole Levo- is the levo-isomer of Ornidazole. Ornidazole is a 5-nitroimidazole derivative with antiprotozoal and antibacterial properties against anaerobic bacteria. Ornidazole Levo- is the less active isomer.
Metronidazole is a nitroimidazole antibiotic medication used particularly for anaerobic bacteria and protozoa.Target: Antibacterial; AntiparasiticMetronidazole is a nitroimidazole antibiotic medication used particularly for anaerobic bacteria and protozoa. Metronidazole is an antibiotic, amebicide, and antiprotozoal.[1] It is the drug of choice for first episodes of mild-to-moderate Clostridium difficile infection [2]. Metronidazole, taken up by diffusion, is selectively absorbed by anaerobic bacteria and sensitive protozoa. Once taken up by anaerobes, it is non-enzymatically reduced by reacting with reduced ferredoxin, which is generated by pyruvate oxido-reductase. Many of the reduced nitroso intermediates will form sulfinamides and thioether linkages with cysteine-bearing enzymes, thereby deactivating these critical enzymes. As many as 150 separate enzymes are affected.In addition or alternatively, the metronidazole metabolites are taken up into bacterial DNA, and form unstable molecules. This function only occurs when metronidazole is partially reduced, and because this reduction usually happens only in anaerobic cells, it has relatively little effect upon human cells or aerobic bacteria.[3]
Eprinomectin(MK-397) is an avermectin selected for development as a topical endectocide; has anthelmintic, insecticidal and miticidal activity.
AN7973 is an benzoxaborole compound, AN7973 blocks intracellular parasite development and inhibits the two Cryptosporidium species (C.parvum and C.hominis) as an Cryptosporidium growth inhibitor[1].
Bithionol 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].
Oxibendazole is a broad-spectrum anthelmintic Target: AntiparasiticOxibendazole is a benzimidazole drug that is used to protect against roundworms, strongyles, threadworms, pinworms and lungworm infestations in horses and some domestic pets. It is usually white to yellowish in appearance, and may take the form of a powder or a tablet. From Wikipedia.
Pentamidine Dihydrochloride(MP601205 dihydrochloride) is an antimicrobial agent.Target: AntiparasiticPentamidine Dihydrochloride 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].
Artemisinin is an anti-malarial drug isolated from the aerial parts of Artemisia annua L. plants.
Cycloguanil, the active metabolite of Proguanil, acts on malaria schizonts in erythrocytes and hepatocytes[1].
NSC5844 is a 4-aminoquinoline derivative, with antitumor and antimalarial activity.
Albendazole D3 is the deuterium labeled Albendazole, which is a member of the benzimidazole compounds used as a drug indicated for the treatment of a variety of worm infestations[1].
Panidazole is an amoebicide.
Fenchlorphos is used to prevent and cure the parasitic in veterinary medicine.
N-Desethyl amodiaquine is the major biologically active metabolite of Amodiaquine. N-Desethyl amodiaquine is an antiparasitic agent. IC50 values for strains V1/S and 3D7 are 97 nM and 25 nM, respectively[1].
Ronidazole is an antiprotozoal agent.Target: AntiparasiticRonidazole is an antiprotozoal agent used in veterinary medicine. It may also have use for the treatment of Tritrichomonas foetus infection in cats. Ronidazole kills T foetus at concentrations > 0.1 μg/mL in vitro. Ronidazole (30 or 50 mg/kg) cures T foetus infection for follow-up durations of 21 to 30 weeks after treatment in 10/10 cats [1].
Cycloguanil hydrochloride, the active metabolite of Proguanil, acts on malaria schizonts in erythrocytes and hepatocytes[1].