antitrypanosomal agent 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 12, a C20-phenylthiourea, exhibits trypanocidal and cytotoxic activities, demonstrating antitrypanosomal activity with GI50 values of 0.22 μM. It induces faster cell swelling in bloodstream-form trypanosomes compared to Salinomycin [1].

Compound 4b (antitrypanosomal agent 13) is a potent antitrypanosomal with notable trypanocidal and cytotoxic activities, exhibiting GI50 values of 0.18 μM against T. brucei and 8.4 μM for HL-60 [1].

Antitrypanosomal agent 14 (Compound 1), a potent T. brucei inhibitor with an effective concentration (EC50) of 0.47 μM, also inhibits Tb GSK3 with an inhibitory concentration (IC50) of 12 μM, and is utilized in the research of Human African Trypanosomiasis [1].

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].

Compound 18 (compound 8b), a nitrofuran derivative, exhibits potent in vitro trypanocidal activity, with an IC50 value of 0.03 μM [1].

Compound 17 (Compd 7a) exhibits potent antiamastigote activity, demonstrated by its IC50 value of 0.03 μM against the T. congolense strain IL3000 [1].

Antitrypanosomal agent 16 functions as a potent trypanocide, exhibiting an inhibitory concentration 50 (IC50) of 0.04μM against the T. congolense strain IL3000 [1].

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.

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

NPD-2975 (compound 30) is an orally active antitrypanosomal agent effective against Human African Trypanosomiasis (HAT), demonstrating acceptable metabolic stability and low toxicity potential in human MRC-5 lung fibroblasts, as well as in an acute mouse model of T. b. brucei infection. It exhibits an in vitro IC50 of 70 nM against T. b. brucei and IC50 values of 0.16 μM and 0.42 μM against CYP1A2 and CYP2C19 enzymes, respectively [1].