t. brucei

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.

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.

CRK12-IN-1 is a potent CRK12 inhibitor with insecticidal activity and exhibits inhibitory effects on Trypanosoma brucei (T.b. brucei) and Trypanosoma congolense (T. congolense) with EC50s of 1.3 and 18 nM, respectively, rapidly killing the pathogenic cells.

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).

Jaspamycin is a potent PKA activator that binds to the PKAR site of Trypanosoma brucei, with EC₅₀ and Kd values of 6.5 nM and 8 nM, respectively. It does not bind to purified human PKARIα and shows favorable antiparasitic activity.

NPD1335, a potent inhibitor of Trypanosoma brucei phosphodiesterase B1 (TbrPDEB1), exhibits submicromolar activity against T. brucei parasites and an improved cytotoxicity profile. By elevating intracellular cAMP levels, NPD1335 disrupts the cell cycle, leading to cell death [1].

Tuberculosis inhibitor 1 is a potent, non-cytotoxic inhibitor of Trypanosoma brucei growth [EC50: 5 nM].

DNA crosslinker 6 (compound 1) is an anti-mitotic agent known for its strong binding affinity to AT-DNA and inhibition of AT-hook 1 binding to DNA (IC50=0.03 µM). Additionally, it exhibits anti-protozoal activity, effectively inhibiting T. brucei with an EC50 of 0.83 µM.

Proteasome-IN-6 (Compound J-80) inhibits the β5 catalytic subunit of the Trypanosoma brucei 20S proteasome, effectively blocking T. b. brucei, T. b. gambiense, and T. b. rhodesiense with EC50 values of 157 nM, 220 nM, and 156 nM, respectively. Additionally, Proteasome-IN-6 has demonstrated antitrypanosomal activity in a mouse model.

PFK-IN-1 (compound 1) is an inhibitor of 6-phosphofructo-1-kinase (PFK), demonstrating IC50 values of 0.41 and 0.23 μM against T. brucei and T. cruzi PFK, respectively, and an ED50 of 15.18 μg/mL for T. brucei. The compound has a half-life of 9.7 minutes in rat liver microsomes and 408 minutes in mouse liver microsomes.

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.

NEU-1017 serves as a broad-spectrum antiparasitic compound, effectively inhibiting T. brucei, L. major, and P. falciparum with EC50 values of 210 nM, 240 nM, and 3 nM, respectively.

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

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.

PEX5-PEX14 PPI-IN-3 (Compound 7) is an inhibitor of the PEX5-PEX14 protein-protein interaction, with an EC50 of 95 μM. It demonstrates an EC50 of 7.2 μM against Trypanosoma brucei and exhibits low cytotoxicity in HepG2 cells. PEX5-PEX14 PPI-IN-3 also possesses antiparasitic activity.

HAT-IN-10 (Compound 12a) is an agent that combats Human African Trypanosomiasis (HAT), with an EC50 value of 0.23 μM against T. brucei. It is useful for HAT research.

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.

GSK2188764 is an inhibitor of T. brucei IPMK, partially inhibits rTbIPMK activity.

Megazol is a nitroimidazole based drug that cures some protozoan infections. A study of nitroimidazoles found the drug extremely effective against T. cruzi and T. brucei which cause Chagas disease and African sleeping sickness, respectively.

NEU-1045 is a T. brucei proliferation inhibitor, and is a promising lead with cross-pathogen activity. NEU-1045 inhibited T. brucei, T. cruzi, and L. major proliferation with good potency (T. brucei EC50 = 0.37 μM; T. cruzi EC50 = 2.8 μM; L. major EC50 =

NEU-1923 is a potent inhibitor of T. brucei proliferation (EC50= 0.37 μM).

NEU-730, a novel inhibitor of TbrPDEB1, shows modest inhibition of T. brucei proliferation.

1. Lycobetaine (Ungeremine) is a potential biofungicide against Penicillium roqueforti and Aspergillus niger.2. Lycobetaine have strong antibacterial activity against Flavobacterium columnare . 3. Lycobetaine effectively targets mammalian as well as bacterial type I and type II topoisomerases.4. Lycobetaine shows strong acetylcholinesterase inhibitory activity(IC(50) value of 0.35 microM). 5. Lycobetaine has antiprotozoal activity, it shows good activity in in vitro assays against Trypanosoma brucei rhodesiense, T. cruzi.