trypanosoma

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

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.

Moxipraquine is a novel 8-aminoquinolone compound with anti-infective activity against Trypanosoma cruzi. Moxipraquine effectively inhibited parasitemia but did not eradicate infections in mice or guinea pigs. Moxipraquine was effective against experimental infections of Leishmania major, Lactobacillus mexicanus, and Lactobacillus brasiliensis, but was Ineffective.

Jaspamycin (7-CN-7-C-Ino) does not bind with purified human PKARIα but exhibits anti-parasite activity and is a potent activator of PKA, binding to the R site (PKAR) with an EC50 of 6.5 nM and a Kd of 8 nM in Trypanosoma brucei.

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

1. Columbin has anti-inflammatory activity. 2. Columbin has chemopreventive ability against human colon cancer. 3. Columbin inhibits PLA2 hydrolysis of ghost RBC in a dose-dependent fashion.

Veraguensin is derived from Magnolia sp.. Veraguensin inhibits bone resorption and shows high antileishmanial activity.

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.

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

6'-hydroxydihydrocinchonidine is a metabolite of quinine, with antimicrobial and antitumor activity, and inhibitory effect on Trypanosoma brucei and Streptococcus pneumoniae.

(2E)-3-(1,3-Benzodioxol-5-yl)-2-propenoic acid displays EC50 values of 73.5 μM against T. cruzi. trypomastigotes.

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.