trypanosoma

Ajugol (Leonuride) shows some trypanocidal potential against Trypanosoma brucei rhodesiense (IC50 values 29.3–73.0 ug/ml).

T.cruzi-IN-1 (MDK1088) is a Trypanosoma cruzi inhibitor.

Anti-Trypanosoma cruzi agent-6 (Compound 8) exhibits inhibitory activity against Trypanosoma cruzi. It effectively suppresses the epimastigote, trypomastigote, and amastigote forms of T. cruzi, with IC50 values of 24.7 µM, 1.8 µM, and 1.6 µM, respectively.

Anti-Trypanosoma cruzi agent-7 (compound 1) is a potent Trypanosoma cruzi inhibitor with an EC50 of 1.26 µM. This compound is used in the study of Chagas disease.

Anti-Trypanosoma cruzi agent-1 (Compd 3b), a selective compound against NINOA trypomastigote (IC 50 = 0.51 μM) and INC-5 epimastigote (IC 50 = 3.06 μM), also possesses anti-T. gondii activity [1].

Anti-Trypanosoma cruzi agent-1 (Compd E5) demonstrates a potent anti-Toxoplasma effect.

Anti-Trypanosoma cruzi agent-3 is an antiprotozoal agent.

Anti-Trypanosoma cruzi Agent-4 is a Trypanosoma cruzi inhibitor utilized for the investigation of infections caused by this parasite.

Antitrypanosomal agent 2 shows potent and specific antiparasite activities against Trypanosoma brucei.

Compound C-1 (Antitrypanosomal agent 21) serves as an inhibitor of Trypanosoma brucei. It effectively reduces the levels of D6XM23 in the parasite lysate.

Antitrypanosomal agent 23 is an antiparasitic compound effective against intracellular amastigotes of Trypanosoma cruzi in LLC-MK2 and C2C12 cells, demonstrating activity with IC50 values of 0.10 and 0.11 μM, respectively. It also acts as a weak inhibitor of recombinant Trypanosoma cruzi sialyltransferase (TcTS) with an IC50 of 1.1 mM.

Antitrypanosomal agent 19 (compound 10) is an orally active antitrypanosomal drug. It effectively inhibits the growth of Trypanosoma brucei brucei, T. b. gambiense, and T. b. rhodesiense, alleviating the acute infection induced in mice by African human trypanosomiasis (HAT).

Antitrypanosomal agent 26 (Compound 1) is an allosteric inhibitor of trypanosome alternative oxidase (TAO). It exhibits potent activity against African trypanosomes, such as Trypanosoma brucei, with an IC50 value of 1.3 nM for recombinant TAO. The compound disrupts the mitochondrial electron transport chain of trypanosomes and inhibits glucose-dependent respiration. Antitrypanosomal agent 26 shows potential for research in treating African animal trypanosomiasis, including bovine trypanosomiasis.

Antitrypanosomal agent 4 (compound 19) is a potent antitrypanosomal compound that crosses the blood-brain barrier and exhibits strong resistance to Trypanosoma cruzi and T. b. brucei with IC50 values of 1.2 μM and 70 nM, respectively.

The antitrypanosomal agent 8 (compound 3b) demonstrated a potent effect against Trypanosoma brucei with an IC50 of 0.79 μM, while the IC50 value was 80.95 μM.

Antitrypanosomal agent 6 (compound 18a) is a potent antitrypanosomal agent demonstrating good ADME properties, with an IC50 of 0.47 μM against Trypanosoma brucei (T. brucei), making it more than twice as active as Nifurtimox; it also exhibits a strong interaction with and selective binding to AT-rich DNA.

Antitrypanosomal agent 10, an antitrypanosomal compound, effectively inhibits Trypanosoma cruzi with an IC50 of 0.28 μM.

Antitrypanosomal Agent 11 is a chemical compound effective against Trypanosoma cruzi, exhibiting an inhibition concentration (IC 50) of 0.23 μM.

Antitrypanosomal Agent 15 (Compound 26) is an orally active, brain-penetrant, selective inhibitor of the Trypanosoma cruzi proteasome, exhibiting a pIC50 of 7.4 for T. cruzi and <4 for the human proteasome. It possesses favorable ADME properties, rendering it useful for the study of Chagas disease [1].

Antitrypanosomal agent 1 is a potent and selective trypanothione reductase (TR) inhibitor (IC50: 3.3 μM) that also inhibits glutathione reductase (IC50: 64.8 μM) and T. brucei (EC50: 1 μM).

Antitrypanosomal agent 20 (Compd 27) is a medication used to combat trypanosome infections, exhibiting an IC50 value of 0.75 μM against T. b. brucei.

Antitrypanosomal agent 24 is a benzothiazole amidoxime compound with potent and selective activity against trypanosomes (IC50 = 0.92 μM). It serves as a substrate for the P-glycoprotein efflux pump and exhibits high membrane permeability and good metabolic stability. Antitrypanosomal agent 24 binds to DNA/RNA via intercalation.

The Antitrypanosomal agent 7 (compound 18c) is a potent anti-trypanosome agent and shows good ADME properties. The Antitrypanosomal agent 7 was more than two-fold more active against T. brucei (IC50: 0.71 μM) than Nifurtimox. Antitrypanosomal agent 7 has a strong interaction with DNA and can selectively bind to AT-rich DNA.

Antitrypanosal agent 5 is a selective anti-trypanosomal agent that acts on T. brucei (IC50: 1 nM) and HEK293 cells (IC50: 483.3 μM).