african trypanosomiasis

DDD85646 is an inhibitor of T. brucei N-myristoyltransferase with a Ki of 1.44 nM, an IC50 of 2 nM and an EC50 of 2 nM. The IC50 of hNMT is 4 nM.

NMT-IN-1 is a potent inhibitor of N-nutyltransferase (NMT), with IC50 of 31μM for TbNMT and 66μM for hNMT. NMT-IN-1 is a potential compound for the treatment of African trypanosomiasis.

Acoziborole (SCYX-7158), a derivative of benzoxaborole, is a safe, effective and structurally novel antigen-worm agent for human African trypanosomiasis (HAT) studies. The MIC value of Acoziborole for T. b. brucei S427 was 0.6 µg/mL.

Eflornithine (DFMO) is a selective and orally available ornithine decarboxylase inhibitor that delays hair overgrowth.Eflornithine is used in the study of African trypanosomiasis, malignant glioma, and sleeping sickness.

JC-229 is a potent and selective TbRPA1 inhibitor that can inhibit RPA1 in Trypanosoma brucei. JC-229 can be used to study human African Trypanosomiasis (HAT).

Potassium 1,2-naphthoquinone-4-sulphonate (Compound 16) acts as an inhibitor of 6-phosphogluconate dehydrogenase (6PGDH) with an IC50 of 53 μM. This compound is applicable in research related to human African trypanosomiasis.

Pafuramidine is an orally bioavailable prodrug of formamidine which was developed for the treatment of human African trypanosomiasis.

S-MGB-234 is a novel Minor Groove Binder that cures animal African trypanosomiasis in an in vivo mouse model. S-MGB-234 has significant potential as novel therapeutic agents for animal African trypanosomiasis.

S-MGB-234 is a minor groove binder used for treating Animal African Trypanosomiasis (AAT). It shows exceptional in vitro efficacy against the main causative agents, Trypanosoma congolense and Trypanosoma vivax, without demonstrating cross-resistance with existing diamidine drugs and is not internalized through the transporters used by diamidines.

Eflornithine hydrochloride, a specific and irreversible inhibitor of ornithine decarboxylase enzyme, is a medication used for the treatment of African trypanosomiasis and excessive facial hair growth in women.

20S Proteasome-IN-4 (Compound 7) is an orally active inhibitor of the 20S proteasome, selectively targeting the parasite form and demonstrating brain penetration capabilities. It exhibits a potent IC50 value of 6.3 nM against the T. b. brucei 20S proteasome, making it suitable for human African trypanosomiasis (HAT) research [1].

GNF6702 is a selective inhibitor of the kinetoplastid proteasome, demonstrating efficacy against parasites in mouse models of leishmaniasis, Chagas disease, and human African trypanosomiasis.

Antitrypanosomal agent 9 is a potent compound with inhibitory activity against T. b. brucei, exhibiting an IC50 of 1.15 μM. It is utilized in research for human African trypanosomiasis (HAT).

HAT-IN-8 (Compound 38), a blood-brain barrier-permeable inhibitor of Trypanosoma brucei with an EC50 of 0.18 μM, is utilized in the study of Human African trypanosomiasis [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].

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].

Kolavenol shows a trypanocidal activity with an IC50 value of 2.5 microg/ml (8.6 microM) against Trypanosoma brucei rhodesiense, the causing agent of the acute form of human African trypanosomiasis.