Parasite

Doxycycline (Doxiciclina) belongs to the tetracycline class of antibiotics and is a broad-spectrum metalloproteinase (MMP) inhibitor with oral activity. Doxycycline has antibacterial activity and antitumor activity.

Lotilaner is a parasiticide. It is used as a potent non-competitive antagonist of insects GABACl receptors (IC50 of 23.84 nM for Drosophila melanogaster GABA receptor). It also has no effect on a dog GABAA receptor.

Suramin Sodium Salt (BAY-205) is a sodium salt form of suramin, a polysulphonated naphthylurea with potential antineoplastic activity. Suramin blocks the binding of various growth factors, including insulin-like growth factor I (IGF-I), epidermal growth factor (EGF), platelet-derived growth factor (PDGF), and tumor growth factor-beta (TGF-beta), to their receptors, thereby inhibiting endothelial cell proliferation and migration. This agent also inhibits vascular endothelial growth factor (VEGF)- and basic fibroblast growth factor (bFGF)-induced angiogenesis; retroviral reverse transcriptase; uncoupling of G-proteins from receptors; topoisomerases; cellular folate transport; and steroidogenesis.

Kaempferol (Robigenin) is a natural flavonoid and an inverse agonist of ERRα and ERRγ. Kaempferol has a wide range of antitumor, anti-inflammatory, antioxidant, antibacterial and antiviral activities.

SQ109 (NSC-722041) is an effective inhibitor of the trypomastigote form of the parasite (IC50 = 50 nM). SQ109 is an antitubercular agent and targets MmpL3.

DDD85646 is an inhibitor of T. brucei N-myristoyltransferase with a Ki of 1.44 nM, an IC50 of 2 nM and an EC50 of 2 nM. The IC50 of hNMT is 4 nM.

Obatoclax Mesylate (GX15-070) is a Bcl-2 antagonist (Ki: 0.22 μM) and can induce apoptosis with up-regulation of Bim, induced cytochrome c release, and activation of caspase-3.

Licoflavone B has schistosomicidal activity, it showed high S. mansoni ATPase (IC50 of 23.78 μM) and ADPase (IC50 of 31.50 μM) inhibitory activities.

RR-11a analog (aza-peptide Michael acceptor, 7a) is an inhibitor of asparaginyl endopeptidase with IC50s of 4.5 nM, 4.5 nM and 31 nM for AE1 in Trichomonas Vaginalis, AE in Ixodes ricinus and AE in Schistosoma mansoni, respectively.

Halofuginone specifically inhibits collagen type I gene expression and matrix metalloproteinase 2 (MMP-2) gene expression, which may result in the suppression of angiogenesis, tumor stromal cell development, and tumor cell growth. Halofuginone Hydrobromide is the hydrobromide salt of halofuginone, a semisynthetic quinazolinone alkaloid anticoccidial derived from the plant Dichroa febrifuga, with antifibrotic and potential antineoplastic activities. These effects appear to be due to halofuginone-mediated inhibition of the collagen type I and MMP-2 promoters. Collagen type I and MMP-2 play important roles in fibroproliferative diseases.

N-Desethyl amodiaquine dihydrochloride is an antiparasitic agent and the major biologically active amodiaquine metabolite. Its IC50 values against strains V1 S and 3D7 were 97 nM and 25 nM, respectively.

RRx-001 is a potent inhibitor ofglucose 6-phosphate dehydrogenase(G6PD) and with potent antimalarial activity

Lupenone is a natural product isolated from Rhizoma Musae and has good anti-diabetic activity,and has anti-inflammatory activity.lupenone were potent PTP1B inhibitors with IC50 values of 15.11±1.23μM.

Sarolaner (PF-6450567) is an orally active, broad-spectrum ectoparasiticide with an LC80 of 0.3 μg mL against C. felis and an LC100 of 0.003 μg mL against O. turicata.

Modoflaner is an antiparasitic (veterinary use).

Daphnetin (7,8-Dihydroxycoumarin), a natural coumarin derivative, is a protein kinase inhibitor with inhibitory for EGFR (IC50: 7.67 μM), PKA (IC50: 9.33 μM), and PKC (IC50: 25.01 μM), also exhibit anti-oxidant and anti-inflammatory activities.

ZY-19489 is an antimalarial compound that is a potential single-dose cure for Plasmodium falciparum and Plasmodium vivax malaria. It has received orphan drug designation from the FDA.

CRK12-IN-2 is a potent inhibitor of CRK12.CRK12-IN-2 inhibits the parasite, with EC50 values of 3.2 and 0.08 nM for Trypanosoma congolense and Trypanosoma vivax, respectively.CRK12-IN-2 can be used for the prevention and treatment of trypanosomiasis in animals.

LeuRS-IN-1 hydrochloride is an orally active and highly potent inhibitor of Mycobacterium tuberculosis leucyl-tRNA synthetase with anti-leukemic activity and anti-malarial activity, inhibits M.tb LeuRS, inhibits HepG2 protein synthesis, and can be used in the study of leukemia.

Fluralaner (A1443) is an isoxazoline ectoparasiticide. It potently and selectively inhibits binding of the GABA receptor channel blocker EBOB to housefly head membranes (IC50: 455 pM).

α-Thujone is an inhibitor of ACh with an IC50 value of 24.7μM.

Amodiaquine is a synthetic aminoquinoline, used to treat malaria.

Allopurinol riboside is a metabolite of allopurinol with potency against parasites. Allopurinol riboside competitively inhibits the action of purine nucleoside phosphorylase on inosine with a Ki of 277 μM.

UCB7362 (GLXC-26743) is an orally available and potent plasmepsin X (PMX) inhibitor with anti-malarial activity.UCB7362 inhibits parasite reproduction.

Avermectin B1a is a macrocyclic lactone disaccharide anthelmintic agent .

Halofuginone (RU-19110), the competitive inhibitor of prolyl-tRNA synthetase(Ki=18.3 nM), could also down-regulate Smad3 and blocked TGF-β signaling at 10 ng ml in the mammal.

Afoxolaner is an isoxazoline insecticide acaricide against Ixodes scapularis in dogs. Afoxolaner acts on the insect GABA and glutamate receptors, inhibiting GABA & glutamate-regulated uptake of chloride ions, resulting in excess neuronal stimulation and death of the arthropod.

Hydroxychloroquine sulfate (Acidum iopanoicum) inhibits plasmodial heme polymerase. It is a chemotherapeutic agent that acts against erythrocytic forms of malarial parasites. Hydroxychloroquine appears to concentrate in food vacuoles of affected protozoa.

Bruceine A (NSC-31616)(NSC-310616; Dihydrobrusatol) is a natural quassinoid compound extracted from the dried fruits of Brucea javanica (L.); are potential candidates for the treatment of canine babesiosis.

1. Dehydrocorydaline (13-Methylpalmatine) exerts anti-metastatic potential via suppression of MMPs and Bcl-2 signaling in NSC-LC cells. 2. Dehydrocorydaline stimulates p38 MAPK activation, which can enhance heterodimerization of MyoD and E proteins, thus resulting in MyoD activation and myoblast differentiation. 3. Dehydrocorydaline shows antiplatelet effects, it inhibits thrombin-induced platelet aggregation in a low dose ( IC50= 34.914 ug mL). 4. Dehydrocorydaline has anti-inflammatory and antinociceptive effects. 5. Dehydrocorydaline inhibits MCF-7 cell proliferation by inducing apoptosis mediated by regulating Bax Bcl-2, activating caspases as well as cleaving PARP.

Fosravuconazole L-lysine ethanolate (BMS-379224 L-lysine ethanolate) is a broad-spectrum antifungal agent approved in Japan for treating onychomycosis, a fungal nail infection. It is a prodrug converted into ravuconazole.

A-484954 (A 484954) is a highly specific eukaryotic elongation factor-2 (eEF2, IC50: 280 nM) inhibitor.

Methylene Blue (Tetramethylthionine chloride) (IC50 of 1.9 μM) inhibits tau filament formation. And it inhibits soluble guanylyl cyclase. It is also used as a dye in chromoendoscopy.

DNDI-6148 has anti-experimental cutaneous leishmaniasis activity and can be used to study visceral leishmaniasis by inhibiting Leishmania protozoa cleavage and polyadenylation-specific factor (CPSF3) endonuclease.

Niclosamide (Niclocide)(BAY2353) is used to treat most tapeworm infections by inhibiting DNA replication.

1. Bruceine D from Brucea javanica, may have the potential to be used as a natural viricide, or a lead compound for new viricides. 2. Bruceine D inhibits the growth of three pancreatic cancer cell lines, i.e., PANC-1, SW199 and CAPAN-1; induces cytotoxicity in Capan-2 cells via the induction of cellular apoptosis involving the mitochondrial pathway.

Toltrazuril sulfone (Ponazuril) is an antiprotozoal agent that acts upon Coccidia parasites.

Diloxanide furoate (Dichlofurazol) is an antiprotozoal compound with oral activity that can be used in the study of amoebas in tissues and several other protozoal infections.

Flubendazole (Flumoxane) is available OTC in Europe that is an anthelmintic using to treat worm infection in humans.

Ascomycin (Immunomycin)(Immunomycin, FR-900520, FK520) is an ethyl analog of tacrolimus (FK506) with strong immunosuppressant properties.

GSK3186899 is an inhibitor of Cdc2-related kinase 12 with an EC50 of 1.4 μM for L. donovani.

Sanguinarine chloride (Pseudochelerythrine chloride), a benzophenanthridine alkaloid, stimulates apoptosis by activating the production of reactive oxygen species (ROS).

N-p-trans-Coumaroyltyramine is a natural product and an acetylcholinesterase (AChE) inhibitor with an IC50 of 122 μM. It also exhibits anti-trypanosomal activity with an IC50 of 13.3 μM for T. brucei rhodesiense.

Quinacrine dihydrochloride (Mepacrine dihydrochloride) is the dihydrochloride salt of the 9-aminoacridine derivative quinacrine with potential antineoplastic and antiparasitic activities.

Hydroxychloroquine (2-[[4-[(7-Chloroquinolin-4-yl)amino]pentyl](ethyl)amino]ethanol) (HCQ) is an alkalinizing lysosomatropic drug that acts by inducing apoptosis of renal cancer cells in vitro and inhibiting TLR7 9. It is a medication used to prevent and treat malaria, and it's also being studied as an experimental treatment for COVID-19.

Isofebrifugine is an alkaloid from the plant Changshan of the Saxifrage family with antimalarial and anti-infectious activity.

D-Phenothrin ((-)-trans-Phenothrin) is a type II synthetic pyrethroid extensively employed in veterinary medicine for pest control on animals, crop protection, and the elimination of insects, mosquitoes, and human lice.

Pentamidine is an antifungal and antiprotozoal agent, interacting directly with the pathogen genome by binding to AT-rich regions of duplex DNA and the minor groove of DNA, thereby interfering with DNA replication.