parasitic

Anti-parasitic agent 3 is effective against drug-resistant parasites.

Primaquine diphosphate is the phosphate salt form of primaquine, a synthetic, 8-aminoquinoline derivative with antimalarial properties. Although its mechanism of action is unclear, primaquine bind to and alter the properties of protozoal DNA. This agent eliminates tissue (exo-erythrocytic) malarial infection, preventing the development of the erythrocytic forms of the parasite which are responsible for relapses in Plasmodium vivax and ovale malaria. Primaquine is active against late hepatic stages (hypnozoites, schizonts).

Paromomycin binds specifically to the RNA oligonucleotide at the A site of bacterial 30S ribosomes, thereby causing misreading and premature termination of translation of mRNA and inhibition of protein synthesis followed by cell death. Paromomycin Sulfate (Aminosidine sulfate) is the sulfate salt form of paromomycin, a structural derivative of neomycin, an aminoglycoside antibiotic with amebicidal and bactericidal effects against predominantly aerobic gram-negative bacteria.

Diclazuril (R-64433) is a coccidiostat.

Nitazoxanide (NSC-697855) is a synthetic benzamide with antiprotozoal activity. Nitazoxanide exerts its antiprotozoal activity by interfering with the pyruvate ferredoxin/flavodoxin oxidoreductase dependent electron transfer reaction.

Arecoline hydrobromide (Arecoline HBr) is a muscarinic acetylcholine receptor agonist.

Asparagusic acid is unique to asparagus. It is responsible for the odorous urine excreted after eating asparagus. Its derivatives ihydroasparagusic acid have an anti-inflammatory effect.

Pyrantel pamoate (Pyrantel embonate) is a depolarizing neuromuscular blocking agent. This compound is commonly used as an anthelmintic to treat parasitic worm infections, effectively paralyzing nematodes by inhibiting their neuromuscular activity.

Chalcone (Cinnamophenone) is an aromatic ketone that forms the central core for a variety of important biological compounds, which are known collectively as chalcones.

Pyrantel tartrate (Banminth) is broad spectrum anthelmintic for livestock.

Stylopine is a protoberberine-type alkaloid that has potential biological activities, including anti-inflammatory activity.

Antiparasitic agent-29 (Compound 5) is a trypanosome alternative oxidase (TAO) inhibitor with an IC50 of 1.3 nM in Trypanosoma brucei. It exhibits broad-spectrum antiparasitic activity against Trypanosoma and Leishmania species. Antiparasitic agent-29 accumulates in parasite mitochondria, selectively disrupting their energy metabolism, and displays strong membrane perturbation activity without cross-resistance. It is useful for research on parasitic diseases such as surra and dourine.

Antiparasitic agent-10 (Compound 94) is a potent anti-parasitic agent with significant anti-schistosomal activity, particularly against adult Schistosoma mansoni, making it a promising candidate for Schistosomiasis research as a treatment option [1].

Antiparasitic Agent-20 (Compound 1p) exhibits broad-spectrum activity as a parasitic inhibitor, demonstrating efficacy against T. brucei and T. cruzi with EC50 values of 0.09 µM and 14.1 µM, respectively [1].

Antiparasitic agent-24 (Compound 14a) is an antiparasitic compound with EC50 values of 0.005 μM for L. maj, 0.069 μM for L. don, 0.82 μM for T. brucei, and 4.1 μM for T. cruzi.

Antiparasitic agent-26 (Compound 8) is an antiparasitic compound that effectively inhibits the growth of Naegleria fowleri, with an IC50 of 22.87 μM (trophozoite stage) and 25.16 μM (cyst stage). It exerts its antiparasitic effects by inducing programmed cell death, which includes cytosolic calcium accumulation, mitochondrial membrane potential collapse, ATP synthesis inhibition, ROS accumulation, and chromatin condensation. Antiparasitic agent-26 can be utilized in research on primary amoebic meningoencephalitis (PAM).

Antiparasitic agent-25 (Compounds 11) is an orally active antiparasitic compound. It inhibits the invasion and replication capabilities of parasites and has an irreversible effect on Toxoplasma gondii. The agent significantly reduces the replication rate of Toxoplasma gondii, with an IC50 value of 6.33 μM, and exhibits low cytotoxicity, having a CC50 value of 285 μM.

Antiparasitic agent-21 (compound 28) exhibits selective antiparasitic activity against Naegleria fowleri, with an EC50 of 0.92 μM. Additionally, Antiparasitic agent-21 demonstrates excellent blood-brain barrier permeability.

Antiparasitic agent-22 (Compound 24) is a broad-spectrum antiparasitic compound that inhibits the procyclic form of T. brucei, L. infantum, and L. tropica with IC50 values of 2.41, 5.95, and 8.98 μM, respectively, and the amastigote form of L. infantum with an IC50 of 8.18 μM. It also shows inhibitory activity against the P. falciparum W2 strain with an IC50 of 0.155 μM. Additionally, Antiparasitic agent-22 exhibits low cytotoxicity in THP1 cells, with a CC50 of 64.16 μM.

Antiparasitic agent-27 (Compound 2) is a potent antiparasitic compound targeting Leishmania infantum with an IC50 of 3.1 μM. It induces cell cycle arrest in the G0/G1 phase and enhances reactive oxygen species (ROS) production to trigger programmed cell death, showing promise for visceral leishmaniasis (VL) research.

Antiparasitic agent-28 is an orally active and selective inhibitor of Toxoplasma gondii phenylalanine tRNA synthetase (TgcPheRS), capable of crossing the blood-brain barrier. It effectively inhibits the growth of T. gondii tachyzoites (TgME49-Fluc strain) with an EC50 of 1 nM, as well as alkaline-induced T. gondii bradyzoites (Tg68nLuc strain) with an EC50 of 3 nM, and glutamine-rich medium-induced bradyzoites with an EC50 of 0.1 nM. Antiparasitic agent-28 demonstrates significant anti-toxoplasmosis efficacy in mice infected with TgME49-Fluc tachyzoites and is utilized in studies involving Toxoplasma gondii infections.

Antiparasitic agent-32 (compound M9) is an analogue of Piperaquine and acts as a potent antiparasitic agent targeting plasmodium falciparum lactate dehydrogenase (Pf LDH) with a Pf3D7IC50 of 0.40 μM. It demonstrates significant activity against both the asexual and gametocyte stages of plasmodium falciparum. Its antimalarial effect is achieved through stable and specific non-covalent interactions at the NADH binding site. Antiparasitic agent-32 is applicable in malaria research.

Antiparasitic agent-31 (Compound LC-61) is a potent agent against Leishmania parasites, exhibiting an IC50 of 0.076 µM against intracellular Leishmania.

Antiparasitic agent-39 (Compound 14) is a selective antiparasitic derivative of Deferasirox that reduces mitochondrial membrane potential. It demonstrates antiparasitic activity against T. brucei, T. gambiense, L. Mexicana, T. gondii, B. divergens, and P. falciparum, with EC50 values of 4.2 nM, 10.4 nM, 52.0 nM, 17.0 nM, 41.2 nM, and 54.8 nM, respectively.