antiparasiti

Rapanone (2,5-Dihydroxy-3-tridecyl-[1,4]benzoquinone) is a natural benzoquinone that is a potent and selective inhibitor of human synovial PLA2.

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-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-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.

Antiparasitic agent-4 (compound 4q) exhibits high antiparasitic activity with an IC50 of 8.51 μM for Leishmania infantum (L. infantum) and an IC50 of 2.20 μM for Trypanosoma cruzi (T. cruzi). It is also cytotoxic against HepG2 cells with a CC50 of 18.97 μM [1].

Antiparasitic agent-6 (compound 5b) demonstrates selective antiparasitic activity against Leishmania infantum (L. infantum) with an IC50 of 3.89 μM and exhibits cytotoxicity against HepG2 cells with a CC50 of 13.64 μM [1].

Antiparasitic agent-2 (compound 8a) exhibits potent antiparasitic activity against Leishmania infantum (L. infantum) and Trypanosoma cruzi (T. cruzi) with IC50s of 7.28 μM and 2.30 μM, respectively, and demonstrates moderate cytotoxicity against HepG2 cells with a CC50 of 26.79 μM [1].

Antiparasitic agent-8 (Compound 9) exhibits potent antiparasitic activity against Hymenolepis nana, with low levels of cytotoxicity [1].

Antiparasitic agent-7 (compound 5d) exhibits specific antiparasitic activity against Leishmania infantum (L. infantum) with an IC50 value of 2.85 μM and demonstrates cytotoxicity against HepG2 cells with a CC50 value of 10.61 μM [1].

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-5 (compound 8h) exhibits potent selectivity against Leishmania infantum (L. infantum) with an IC50 value of 2.50 μM and displays cytotoxic effects on HepG2 cells with a CC50 value of 6.78 μM [1].

Antiparasitic agent-9 (compound 47) is a highly effective and orally administered antiparasitic agent, demonstrating significant efficacy against the human parasite [1].

Antiparasitic Agent-14 is a potent antiparasitic compound with demonstrated cytotoxicity and antiparasitic activity, effectively inhibiting the growth of trypomastigote and amastigote forms [1].

Antiparasitic Agent-17 (compound 5u), an orally active antiparasitic, demonstrates inhibition against both Chloroquine-sensitive (Pf3D7) and Chloroquine-resistant (PfK1) strains, with IC50 values of 0.96 μM and 1.67 μM, respectively [1].

Antiparasitic agent-18 (compound 3a) exhibits potent and selective antiprotozoal activity, effectively inhibiting T. brucei (EC50 = 0.4 µM), T. cruzi (EC50 = 0.21 µM), and L. donovani (EC50 = 0.26 µM) [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].