antiparasitic agent 3

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

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.

Antimalarial agent 44 (Compound 3) is an antiparasitic agent effective against malaria. It exhibits good permeability in MDCK-MDR1 cell monolayers and has a high clearance rate in mouse liver microsomes.

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.

Δ²-Avermectin B₁ₐ (Compound 3) is an antiparasitic agent that specifically targets glutamate-gated chloride channels (GluCls) in the neuromuscular systems of invertebrates. By increasing chloride ion influx, it causes depolarization of neuromuscular cell membranes, inhibiting neural signal transmission, which ultimately paralyzes and kills the parasite. It shows potential for research in agricultural pest control.

Anti-infective agent 3 is an antiprotozoal and antimycobacterial agent. Anti-infective agent 3 (compound 3l) exhibits antiparasitic activity against P. falciparum and T. brucei rhodesiense, with IC 50 values of 0.47 and 0.13 μM, respectively. Anti-infective agent 3 exhibits antimycobacterial activity against Mycobacterium smegmatis with a MIC of 4 μg/mL [1].