Ethopabate is an antiprotozoal agent which has been widely used to treat and prevent coccidiosis in chickens.
Ferroquine is an ingenious antimalarial agent.
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.
Artemisone (Artemifone) is a potent and semi-synthetic antimalarial, inhibits P. falciparum strains, with a mean IC50 of 0.83 nM[1].
Albendazole sulfoxide D3 is deuterium labeled Albendazole sulfoxide, which is a broad-spectrum anthelmintic.
Levamisole Hcl is an anthelmintic and immunomodulator belonging to a class of synthetic imidazothiazole derivatives.IC50 value: Target: Levamisole suppresses the production of white blood cells, resulting in neutropenia and agranulocytosis. With the increasing use of levamisole as an adulterant, a number of these complications have been reported among cocaine users [1] [2]. Levamisole reversibly and noncompetitively inhibits most isoforms of alkaline phosphatase (e.g., human liver, bone, kidney, and spleen) except the intestinal and placental isoform [3]. It is thus used as an inhibitor along with substrate to reduce background alkaline phosphatase activity in biomedical assays involving detection signal amplification by intestinal alkaline phosphatase, for example in in situ hybridization or Western blot protocols. It is used to immobilize the nematode C. elegans on glass slides for imaging.
Sarolaner (PF-6450567) is an orally active, broad-spectrum ectoparasiticide, has efficacy against fleas and ticks on dogs, with LC80 of 0.3 μg/mL against C. felis and an LC100 of 0.003 μg/mL against O. turicata[1].
Lumefantrine is an antimalarial drug, used in combination with Artemether. The artemether-lumefantrine (AL) as the first- and second-line anti-malarial drugs.
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]
Toltrazuril is an antiprotozoal agent that acts upon Coccidia parasites.Target: AntiparasiticToltrazuril is an antiprotozoal agent that acts upon Coccidia parasites. Toltrazuril induces changes in the fine structure of coccidian development stages that are mainly due to a swelling of the endoplasmatic reticulum and of the Golgi apparatus and to abnormalities in the peri-nuclear space, disturbance in nuclear division. Treated with toltrazuril showed a considerably lower mean opg to that of group C (5.78 opg versus 144.62 opg) (p < 0.05) and a FOCR of 97.7 %. The higher efficacy (99.23 %) was observed at 15 days post treatment; however, the average efficacy of the drug remained extremely high (> 90 %) for all the study.
Dimetridazole is a nitroimidazole class drug that combats protozoan infections.Target: AntiparasiticDimetridazole (DMZ) is a 5-nitroimidazole drug traditionally used for the prevention and treatment of histomoniasis in turkeys, trichomoniasis in pigeons, genital trichomoniasis in cattle and the prevention and treatment of haemorrhagic enteritis in pigs.
Toltrazuril sulfone is an antiprotozoal agent that acts upon Coccidia parasites.IC50 Value:Target: AntiparasiticPonazuril (INN, Toltrazuril sulfone), sold by the Bayer Corporation under the trade name Marquis, is a drug currently approved for the treatment of equine protozoal myeloencephalitis in horses, caused by Sarcocystis neurona. More recently, veterinarians have been preparing a formulary version of the medication for use in small animals such as cats and dogs against coccidia, an intestinal parasite. Coccidia treatment is far shorter than treatment for EPM. Ponazuril (INN, Toltrazuril sulfone) is useful for Antiprotozoal.
Phenothrin is a synthetic pyrethroid that kills adult fleas and ticks. It has also been used to kill head lice in humans.
Eugenol is an essential oil found in cloves with antibacterial, anthelmintic and antioxidant activity. Eugenol is shown to inhibit lipid peroxidation.
GNF179 is an optimized 8,8-dimethyl IP analog that exhibited the potency(4.8 nM against the multidrug resistant strain W2) in vitro metabolic stability and in vivo oral bioavailability.IC50 value: 4.8 nM [1]Target: Anti-parasitic agent GNF179 exhibits a low clearance (CL=22 ml/min/kg, ~25% of hepatic blood flow in mice), a large volume of distribution (steady-state volume of distribution, Vss=11.8 l/kg), a moderate residence time (MRT=9 hours) and suitable terminal half-life (t1/2=8.9 hours). GNF179 reduced Plasmodium berghei parasitemia levels by 99.7% with a single 100 mg/kg oral dose, and prolonged mouse survival by an average of 19 days. GNF179 was able to protect against an infectious P. berghei sporozoite challenge with a single oral dose at 15 mg/kg while NITD609 was not.
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.
Diclazuril is an anti-coccidial drug. Target: AntiparasiticDiclazuril is a coccidiostat, the lambs treated with diclazuril showed an intense, persistent oocyst excretion, with average levels of 97.54 opg, considerably higher than those recorded in the animals treated with toltrazuril (p < 0.05) [1]. Diclazuril is effective against E. maxima later in its life cycle, subclinical intestinal lesions may be present for a short time after infection. Diclazuril was shown in studies to reduce lesion scores and improve performance and health of birds challenged with E. maxima [2].
Piperazine Citrate is an organic compound that consists of a six-membered ring, containting two nitrogen atoms at opposite positions in the ring; first introduced in 1953 as an Anthelmintic.
Nifurtimox, an antiprotozoal agent, which is generally used for the treatment of infections with Trypanosoma cruzi, has been used in the therapy of neuroblastoma. Nifurtimox affects enzyme activity of lactate dehydrogenase (LDH).
Piperazine adipate is a potent broad spectrum anthelmintic against many common worm infections in mammals.
Tilbroquinol is an antiprotozoal agent effective against amoebiasis. It has also been used against Vibrio cholerae.IC50 Value: Target: Antiparasitic
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).
N-Desethyl amodiaquine dihydrochloride is the major biologically active metabolite of Amodiaquine. N-Desethyl amodiaquine dihydrochloride is an antiparasitic agent. IC50 values for strains V1/S and 3D7 are 97 nM and 25 nM, respectively[1].
SQ109 is a potent inhibitor of the trypomastigote form of the parasite, with IC50 for cell killing of 50±8 nM.
Pyrantel tartrate is an antinematodal thiophene; nicotinic receptor agonist and can elicit spastic muscle paralysis in parasitic worms due to prolonged activation of the excitatory nicotinic acetylcholine (nACh) receptors on body wall muscle.
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.