antitrypanosomal agent 2

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 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.

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.